Psoriasis

Disease ID:801
Name:Psoriasis
Associated with:4 targets
2 immuno-relevant targets
56 immuno-relevant ligands
Description
A long-term autoimmune disease characterized by patches of red, itchy, and scaly skin. Five types of psoriasis are recognised: plaque (psoriasis vulgari), guttate, inverse, pustular, and erythrodermic, with plaque psoriasis being the most common type.
Database Links
Disease Ontology: DOID:8893

Targets

C5a1 receptor
Role:  Evidence of a role for C5aR in psoriasis stems from the observation that the ligands for C5aR, C5a/C5a-des-arg, are the most abundant cytokine isolated from human psoriatic scales.
References:  5,40
NLRP1
CD2
Comments:  CD2 is the molecular target of alefacept, a drug that was approved for the treatment of moderate to severe plaque psoriasis.
Ligand interactions: 
Ligand Comments
alefacept
Approved drug for plaque psoriasis (no longer authorised for use in some countries).
CD6
Comments:  CD6 is the molecular target of itolizumab, a drug approved for the treatment of chronic plaque psoriasis.
Ligand interactions: 
Ligand Comments
itolizumab
Approved drug for chronic plaque psoriasis.

Ligands

Key to terms and symbols Click ligand name to view ligand summary Click column headers to sort
Ligand References Clinical and Disease comments
doramapimod
Immuno Disease Comments: Phase 2 clinical candidate for psoriasis.
Clinical Use: Doramapimod (as research code BIRB 796) has been assessed in Phase II clinical trials for plaque-type psoriasis and rheumatoid arthritis (RA). Additional trials for RA and Crohn's disease were terminated. Development of the compound has not progressed beyond Phase II. | View clinical data
Bioactivity Comments: Doramapimod shows moderate selectivity for the p38α, -β and -γ isozymes compared to p38δ [39]. A Kd value of 0.1nM is reported in [44], but the authors do not specify subtype identity. In a screening panel of kinases, doramapimod inhibited many kinases with IC50 values <100nM (see Supplementary Information attached to [39]). | View biological activity
CXCL11 26
Immuno Disease Comments: CXCL11 (and CCL5) expression is increased in lesional compared with nonlesional psoriatic skin, and levels correlate with levels of IFNγ in the skin samples.
guselkumab
Immuno Disease Comments: First anti-IL-23 biologic therapy to be approved. Approved for the treatment of moderate to severe plaque psoriasis, in patients considered as candidates for systemic therapy or phototherapy.
Clinical Use: Having completed Phase III clinical trials for various forms of psoriasis, guselkumab was approved in 2017 for patients with moderate to severe plaque psoriasis. Click here to link to ClinicalTrials.gov's listing of Phase III guselkumab trials. | View clinical data
Bioactivity Comments: Results from an earlier clinical trial indicate that 50-100% of guselkumab-treated patients achieved a 75% improvement in psoriasis area severity index scores12 weeks after a single dose treatment. None of the patients receiving placebo showed any improvement [50]. Decreased epidermal thickness and T-cell and dendritic cell expression was observed in lesional and nonlesional skin biopsies from guselkumab-treated patients compared with placebo-treated patients, indicative of improved disease control [50].
Development of guselkumab is claimed in patent US7935344 [4], where it is likely to be the monoclonal identified as 3759EQ/QS, based on peptide sequence identity. The patent provides a graphical representation of 3759EQ/QS displacement of IL-23 binding to IL-23R (in Figure 10), but does not provide a calculated affinity constant or IC50 value for this binding assay. | View biological activity
mirikizumab
Immuno Disease Comments: Phase 2 clinical candidate for moderate to severe plaque type psoriasis- see NCT02899988.
Clinical Use: Phase 2 clinical trials which will evaluate mirikizumab (as research code LY3074828) in Crohn's disease (NCT02891226), ulcerative colitis (NCT02589665) and plaque psoriasis (NCT02899988) patients are underway. | View clinical data
Bioactivity Comments: Mirikizumab (Antibody I) binds monkey IL-23 with a Kd of 0.056nM, and rabbit IL-23 with a Kd of 53nM, but does not bind rat or mouse IL-23 or human IL-12, IL-27 or IL-35 [3]. Antibody I blocks binding of IL-23 to the IL-23R in vitro, but does not inhibit IL-23 binding to IL-12Rβ1 (the other subunit of the functional IL-23R heterodimer). Effects of Antibody I in vivo are described in the associated patent documentation [3]. | View biological activity
piclidenoson
Immuno Disease Comments: Clinical candidate for plaque psoriasis (Phase 2 NCT00428974).
Clinical Use: Piclidenoson (CF101) is being evaluated in a number of clinical trials, as a potential therapy for several autoimmune-inflammatory disorders (rheumatoid arthritis, Phase III, NCT02647762 [56]; plaque psoriasis, Phase II [8]; uveitis Phase II) and glaucoma (Phase II, NCT01033422 [13]). | View clinical data
GSK2981278 49
Immuno Disease Comments: Phase 2 clinical candidate for plaque type psoriasis (see NCT03004846).
Clinical Use: GSK2981278 has completed Phase 2 clinical trial (NCT03004846) in patients with plaque psoriasis. | View clinical data
Bioactivity Comments: GSK2981278 inhibits activation of the IL17 promoter in a reporter gene assay [49]. Concentrations of GSK2981278 ≥ 3nM leads to almost complete inhibition of IL-17A protein secretion. | View biological activity
tapinarof
Immuno Disease Comments: Phase 3 clinical candidate for plaque psoriasis- NCT03202004.
Clinical Use: Topically applied tapinarof (research code GSK2894512) has shown clinical efficacy in Phase 2 clinical trial in patients with plaque psoriasis [6] (NCT02564042). A Phase 3 trial (NCT03202004) is ready to recruit subjects (Oct 2017). Tapinarof has also completed Phase 1 studies for atopic dermatitis. | View clinical data
Bioactivity Comments: Tapinarof inhibits proinflammatory cytokine expression in vitro and exhibits anti-inflammatory effects in vivo [48]. | View biological activity
CEP-37440
Immuno Disease Comments: Phase 2 clinical candidate for moderate-severe psoriasis- see NCT02931838
Clinical Use: CEP-37440 has completed Phase 1 clinical trial as an oncology candidate (see NCT01922752). | View clinical data
Bioactivity Comments: CEP-37440 inhibits ALK-driven cell proliferation with an IC50 of 22nM, and FAK-driven cells with an IC50 of 82nM [43]. | View biological activity
seletalisib 22
Immuno Disease Comments: Phase 1 clinical candidate for psoriasis- see NCT02303509
Clinical Use: First-in-human results were reported by Helmer et al. (2017) [22]. This article reports data from clinical trials NCT02303509 (safety and tolerability in healthy and psoriatic subjects) and NCT02207595 (safety and tolerability in healthy subjects only). A proof of concept Phase 2 trial in patients with primary Sjögren's syndrome has been terminated due to difficulty in enrolling suitable patient numbers (NCT02610543). | View clinical data
MK-0873
Immuno Disease Comments: Completed Phase 2 trial for plaque psoriasis- see NCT01140061
Clinical Use: MK-0873 has completed Phase 2 clinical evaluation in rheumatoid arthritis (NCT00132769), and Phase 1 as a topical agent for plaque psoriasis (NCT01235728). A Phase 2 trial in patients with chronic obstructive pulmonary disease (COPD) was terminated (NCT00132730). | View clinical data
Bioactivity Comments: MK-0873 inhibits LPS-induced production of TNF-α in human whole blood assays. Only the IC50 of MK-0873 vs. PDE4A is defined in [19], but the authors state less than a 5-fold difference in the IC50 values across the 4 PDE4 isozymes (4A, 4B, 4C and 4D). | View biological activity
CCL2
Immuno Disease Comments: CCL2 is implicated in the pathogenesis of psoriasis.
cortisol
Immuno Disease Comments: Glucocorticoid drug used to treat many inflammatory condtions including psoriasis.
Clinical Use: Hydrocortisone is used to treat many immune and allergic disorders, adrenal insufficiency disorders (eg Addison's disease) and corticosteroid-responsive dermatological disorders (eg psoriasis, atopic dermatitis, and contact dermatitis). | View clinical data
triamcinolone
Immuno Disease Comments: Glucocorticoid drug used to treat many inflammatory condtions including psoriasis.
Clinical Use: Triamcinolone is used for its antiinflammatory or immunosuppressive actions in many conditions. For example, oral triamcinolone is used to treat conditions such as allergic disorders, skin conditions, ulcerative colitis, arthritis, lupus, psoriasis, and breathing disorders. This drug is also used topically as an anti-inflammatory and anti-pruritic agent. Injectable forms of the drug may be used to reduce intra-articular joint pain, stiffness and swelling associated with rheumatoid and osteoarthritic arthritis, bursitis, epicondylitis, and tenosynovitis. | View clinical data
ACTH
Immuno Disease Comments: A corticotropin used to treat the symptoms of many inflammatory disorders including psoriasis.
Clinical Use: Corticotropin is used to treat the symptoms of many allergic disorders, psoriasis and other skin conditions, eye conditions, arthritis, lupus, multiple sclerosis, ulcerative colitis and breathing disorders, for example. This peptide is also used to diagonse adrenocortical insufficiency. | View clinical data
Bioactivity Comments: Although we have recorded affinity data for ACTH at melanocortin receptors 1, 3, 4 and 5, affinity data for the human melanocortin receptor 2, the peptide's primary target, is lacking. As a peptide mimetic of ACTH we would expect corticotropin to have similar affinities to the endogenous peptide. | View biological activity
adalimumab
Immuno Disease Comments: Anti-TNFα monoclonal antibody therapy approved for psoriatic arthritis and plaque psoriasis.
Clinical Use: Used in the management of rheumatoid arthritis, juvenile idiopathic arthritis, psoriatic arthritis, ankylosing spondylitis, Crohn's disease and plaque psoriasis.
In 2015 both the EMA and the FDA approved the use of adalimumab as a treatment for hidradenitis suppurativa, a chronic skin disease that causes abscesses and scarring on the skin.
In July 2016, the FDA expanded adalimumab approval as the first non-corticosteroid drug available for use as a treatment for non-infectious intermediate, posterior and panuveitis (forms of autoimmune-driven inflammation of the uvea)- results from Phase 3 clinical trial NCT01138657 are published in [23]. | View clinical data
IL-17A
Immuno Disease Comments: Approved therapy for psoriasis.
brodalumab
Immuno Disease Comments: Approved therapeutic for plaque psoriasis.
Clinical Use: Brodalumab was first approved in Japan (2016), and by the US FDA for plaque psoriasis the following year. Regulatory decisions are pending elsewhere. Clinical trials for the treatment of psoriatic arthritis (Phase III), moderate to severe plaque psoriasis (Phase III) and asthma (Phase II) are ongoing. Encouraging results from a Phase II study have been reported [36]. | View clinical data
Bioactivity Comments: BLAST searches using the peptide sequences of the heavy and light chains of brodalumab link to patent US7767206 [54], and monoclonal antibody clone AMH14/AML14. | View biological activity
methimazole
Immuno Disease Comments: Approved drug for psoriasis.
Clinical Use: Used in the treatment of hyperthyroidism, goiter, Graves disease and psoriasis. | View clinical data
golimumab
Immuno Disease Comments: An anti-TNFα therapy approved for psoriasis.
Clinical Use: Used in adults with various inflammatory conditions [58] e.g. moderate to severe active rheumatoid arthritis [28], active psoriatic arthritis, active ankylosing spondylitis and moderate to severe ulcerative colitis. | View clinical data
amcinonide
Immuno Disease Comments: A glucocorticoid (corticosteroid) drug used to treat psoriasis.
Clinical Use: Used to treat itching and inflammation associated with allergic and other inflammatory skin conditions. | View clinical data
alefacept
Immuno Disease Comments: Approved drug for plaque psoriasis (no longer authorised for use in some countries).
Clinical Use: This drug was approved for the treatment of inflammation in moderate to severe psoriasis with plaque formation. Use of alefacept has since been discontinued in the US. | View clinical data
Bioactivity Comments: The Miller et al. (1993) article does not provide a calculated IC50 value for LFA3TIP's inhibition of the CD2/LFA-3 interaction [38]. The inhibition is assessed by measuring rosetting of Jurkat/human red blood cells (with an approximate IC50 of 1-5μg/ml of protein from graphical data in Figure 3a), or by measuring inhibition of induced T cell proliferation (with LFA3TIP inhibition at approximately 86%) [38]. | View biological activity
efalizumab
Immuno Disease Comments: Approved drug for psoriasis which was later withdrawn from the market.
Clinical Use: Used to treat psoriasis prior to withdrawl from the market. | View clinical data
Bioactivity Comments: A peptide BLAST search using the heavy chain peptide sequence of efalizumab identifies sequence ID 5 in patent US6703018 [24] and data is presented from the monoclonal variant designated MHM24 F(ab)-8. | View biological activity
etanercept
Immuno Disease Comments: Approved drug for severe plaque psoriasis.
Clinical Use: Used to treat severe active rheumatoid arthritis in adults, severe juvenile idiopathic arthritis, ankylosing spondylitis, and severe plaque psoriasis. | View clinical data
ustekinumab
Immuno Disease Comments: An anti-IL-12B therapy approved to treat psoriasis.
Clinical Use: Used to treat adult patients (18 years or older) with moderate to severe plaque psoriasis who are candidates for phototherapy or systemic therapy and is approved in the US to treat psoriatic arthritis. | View clinical data
Bioactivity Comments: The patent covering the production and use of ustekinumab (US6902734 [16]) does not provide affinity values for specific antibody clones, therefore we have included the stated range of affinities determined in the production and testing process in the interaction table below.. | View biological activity
betamethasone
Immuno Disease Comments: A glucocorticoid (corticosteroid) drug used to treat psoriasis.
Clinical Use: Betamethasone is a synthetic glucocorticoid receptor (GR) agonist, with anti-inflammatory, antipruritic, and vasoconstrictive activities. The drug is used to treat the inflammatory sympotoms of conditions including atopic, seborrhoeic, and contact dermatitis, psoriasis and insect bite reactions. | View clinical data
clobetasol propionate
Immuno Disease Comments: A glucocorticoid (corticosteroid) drug used to treat psoriasis.
Clinical Use: Used to treat skin inflammation and itching caused by conditions such as allergic reactions, eczema, and psoriasis. | View clinical data
desonide
Immuno Disease Comments: A glucocorticoid (corticosteroid) drug used to treat psoriasis.
Clinical Use: Used to reduce skin inflammation caused by allergic reactions, eczema and psoriasis. | View clinical data
Bioactivity Comments: We have been unable to find publicly available affinity data for this drug to substantiate its MMOA, so have not tagged a primary drug target in this case. | View biological activity
desoximetasone
Immuno Disease Comments: A glucocorticoid (corticosteroid) drug used to treat psoriasis.
Clinical Use: Used to reduce skin inflammation caused by allergic reactions, eczema and psoriasis. | View clinical data
diflorasone diacetate
Immuno Disease Comments: A glucocorticoid (corticosteroid) drug used to treat psoriasis.
Clinical Use: Used to reduce skin inflammation caused by allergic reactions, eczema and psoriasis. | View clinical data
flumethasone pivalate
Immuno Disease Comments: A glucocorticoid (corticosteroid) drug used to treat psoriasis.
Clinical Use: Used to reduce skin inflammation caused by allergic reactions, eczema and psoriasis. However, there is no information regarding approval for clinical use of this drug on the US FDA website. Other national approval agencies may have granted marketing authorisation. | View clinical data
ixekizumab
Immuno Disease Comments: Approved therapeutic for psoriasis and plaque psoriasis.
Clinical Use: Ixekizumab is approved for the treatment of psoriasis. Positive results from a Phase 2 study are reported in [15], and Phase 3 results are reviewed in [11]. In March 2016, the US FDA approved ixekizumab for the treatment of moderate-to-severe plaque psoriasis. The EMA granted marketing authorisation in April 2016.
Phase 3 results following 60 weeks of treatment are reported in [17], showing longer term efficacy (with ~80% of patients seeing at least a 75% improvement in their skin symptoms at 60 weeks). | View clinical data
prednicarbate
Immuno Disease Comments: A glucocorticoid (corticosteroid) drug used to treat psoriasis.
Clinical Use: Prednicarbate is a topical corticosteroid drug [20]. It is used to relieve inflammatory and pruritic symptoms of corticosteroid-responsive skin conditions such as seborrheic or atopic dermatitis, localized neurodermatitis, psoriasis, the late phase of allergic contact dermatitis and the inflammatory phase of xerosis cutis. Prednicarbate is claimed to have low atrophogenic potential compared to other glucocorticoids [29,32]. | View clinical data
Bioactivity Comments: We have been unable to find publicly available affinity data for this drug at its proposed molecular target to substantiate its MMOA, and have therefore not tagged a primary drug target. | View biological activity
E6201
Immuno Disease Comments: Phase 2 clinical trial for Psoriasis vulgaris has been completed. More recently, a Phase 1/2 study in FLT3 mutation positive AML has been initiated (NCT02418000).
Clinical Use: E6201 has been assessed in the completed clinical trial NCT01268527, for the treatment of psoriasis vulgaris. There are no further ongoing trials registered with ClinicalTrials.gov (Nov 2014). | View clinical data
Bioactivity Comments: E6201 has significant inhibitory effects on pro-inflammatory cytokine production from various immune cells, and inhibits hyperproliferation of human keratinocytes [18,41,47], activities which underscore its potential as a drug candidate for the treatment of psoriasis. The compound also has potential antineoplastic activity. | View biological activity
sotrastaurin
Immuno Disease Comments: Completed Phase 2 clinical trial NCT00885196 for plaque psoriasis.
Clinical Use: Sotrastaurin (AEB071) has been assessed in a number of clinical trials, for a wide variety of oncology indications, in autoimmune conditions such as plaque psoriasis, and also as an anti-rejection therapy following kidney/liver transplantation. Link here to ClinicalTrials.gov's listing of currently registered sotrastaurin trials. The only open trial (May 2017) is Phase 1 NCT02273219 in uveal melanoma. | View clinical data
secukinumab
Immuno Disease Comments: Approved therapeutic for plaque psoriasis.
Clinical Use: Secukinumab is approved by the US FDA for the treatment of plaque psoriasis.
Secukinumab also met its clinical endpoints in Phase III clinical trial for ankylosing spondylitis (NCT01649375) [2], and was FDA approved for this indication and psoriatic arthritis [35,37] in January 2016.
The antibody is also in Phase II clinical trial for multiple sclerosis (NCT01874340) based on results from experiments in an animal model of the disease (experimental autoimmune encephalomyelitis, EAE) and in vitro human cell assays [10]. | View clinical data
tildrakizumab 45
Immuno Disease Comments: Approved drug for moderate to severe plaque psoriasis.
Clinical Use: Tildrakizumab completed Phase 3 clinical trial for plaque psoriasis (NCT01729754 and NCT01722331), and having shown significant clinical benefit over placebo and and a favourable safety profile [45], was FDA approved in March 2018, for the treatment of phototherapy candidate, adult patients with moderate to severe plaque psoriasis. | View clinical data
itacitinib
Immuno Disease Comments: Phase 2 study NCT01634087 in psoriasis has been completed.
Clinical Use: INCB039110 is being assessed in Phase II clinical trial as a potential treatment for indications such as rheumatoid arthritis (RA), post essential thrombocythemia myelofibrosis, chronic plaque psoriasis and non-small cell lung cancer (NSCLC). | View clinical data
navarixin
Immuno Disease Comments: Completed Phase 2 clinical trial NCT00684593 for psoriasis.
Clinical Use: Navarixin (SCH-527123) has been evaluated in Phase II clinical trials for immune conditions such as allergen-induced asthma, chronic obstructive pulmonary disease (COPD) and psoriasis. | View clinical data
risankizumab
Immuno Disease Comments: Phase 3 clinical candidate for psoriasis.
Clinical Use: Risankizumab has reached Phase II clinical trial for Crohn's disease (CD), psoriasis, and ankylosing spondylitis (AS). Results from the first-in-human proof-of-concept trial in patients with psoriasis are reported in [33]. | View clinical data
ZPL-3893787
Immuno Disease Comments: Completed Phase 2 trial in psoriasis (see NCT02618616).
Clinical Use: ZPL-3893787 has reached Phase 2 clinical trial for evaluation as an antiinflammatory agent in patients with plaque psoriasis (see NCT02618616), and a Phase 1 in atopic dermatitis has been completed. | View clinical data
bimosiamose
Immuno Disease Comments: No progress beyond Phase 2 trial.
Clinical Use: Bimosiamose has completed Phase II clinical trials in patients with chronic obstructive pulmonary disease (COPD; inhaled bimosiamose, NCT01108913 [57]) and psoriasis (topically applied bimosiamose, NCT00823693) | View clinical data
Bioactivity Comments: We do not include the selectins as molecular targets in this database.
Bimosiamose (TBC1269) has a reported IC50 of 70μM in a P-selectin HL-60 cell assay [31]. | View biological activity
timolumab
Immuno Disease Comments: Completed Phase 1 clinical trial NCT00871598.
Clinical Use: Timolumab (with research code BTT1023) is being evaluated in Phase II clinical trial NCT02239211, for its potential to treat patients with primary sclerosing cholangitis, an uncommon and progressive disease of the bile ducts characterised by inflammation and obliterative fibrosis. Phase I studies for RA and psoriasis have been completed (2010/11). | View clinical data
crisaborole
Immuno Disease Comments: Phase 2 clinical candidate for plaque psoriasis.
Clinical Use: Crisaborole (with research code AN2728) has completed Phase 3 clinical trials as a monotherapy for atopic dermatitis (NCT02118792 and NCT02118766) and has received FDA approval for treatment of mild-to-moderate atopic dermatitis in December 2016. | View clinical data
Bioactivity Comments: Inhibits partially purified human PDE4 with an IC50 of 490nM, and inhibits cytokine release in vitro and in vivo [1]. | View biological activity
toreforant
Immuno Disease Comments: No progress beyond Phase 2 trial.
Clinical Use: Toreforant failed to show clinical efficacy in a Phase 2 clinical trial in patients with active rheumatoid arthritis [53]. Phase 2 studies NCT01823016 and NCT02295865 in patients with uncontrolled, persistent asthma and moderate to severe plaque-type psoriasis respectively have been completed. | View clinical data
fezakinumab
Immuno Disease Comments: Completed Phase 1 trial for psoriasis (see NCT00563524).
Clinical Use: Fezakinumab (ILV-094) has reached Phase 2 for atopic dermatitis (NCT01941537 ongoing), rheumatoid arthritis (NCT00883896 completed) and Phase 1 for psoriasis (NCT00563524 completed). | View clinical data
Bioactivity Comments: Fezakinumab shows cross-species reactivity, blocking IL-22 receptor activation and cellular proliferation induced by murine, monkey and rat IL-22 in addition to the human cytokine [14]. | View biological activity
brazikumab
Immuno Disease Comments: No progress beyond Phase 1 trial.
Clinical Use: Phase 1 clinical trials evaluating brazikumab as a monotherapy in mild to severe Crohn's disease (NCT01258205) and moderate to severe psoriasis (NCT01094093) have been completed. Phase 2 trials in subjects with active, moderate to severe Crohn's disease are ongoing (see NCT02574637 and NCT01714726). | View clinical data
Bioactivity Comments: It is unclear which anti-IL-23 antibody in patent WO2011056600 is AMG 139, although antibodies B and E were crystalised to produce X-ray structures, suggesting these were preferred agents [55]. In binding affinity experiments using recombinant human IL-23, all of the chosen antibodies produced equilibrium dissociation constant (KD) values <4pM [55]. | View biological activity
vunakizumab
Immuno Disease Comments: In clinical trial in China.
Clinical Use: Vunakizumab (SHR-1314) does not appear to be registered in any clinical trials with ClinicalTrials.gov. Online searches suggest it is being trialled in China, in patients with psoriasis. | View clinical data
amiselimod
Immuno Disease Comments: Phase 2 clinical candidate for plaque psoriasis.
Clinical Use: Amiselimod (MT-1303) has completed Phase 2 dose-finding clinical trials in patients with relapsing-remitting multiple sclerosis (NCT01742052) and moderate to severe chronic plaque psoriasis (NCT01987843). Phase 2 trials in Crohn's disease patients are underway. | View clinical data
Bioactivity Comments: In vivo (in mice) amiselimod (MT-1303) hydrochloride decreases peripheral blood lymphocyte count with an ED50 value of 0.04mg/kg body weight [30]. Affinity for S1P receptors is not provided in the patent. Note that bioactivity is attributed to the active metabolite [52], the prodrug is almost completely inactive at S1P1R. | View biological activity
itolizumab
Immuno Disease Comments: Approved drug for chronic plaque psoriasis.
Clinical Use: Itolizumab has been licensed India since 2013 as a treatmant for chronic plaque psoriasis [9,25,34]. Itolizumab has also been evaluated in patients with rheumatoid arthritis [46]. | View clinical data
PF-06263276
Immuno Disease Comments: Compelted Phase 1 trial in plaque psoriasis patients (see NCT02193815)
Clinical Use: PF-06263276 was progressed to clinical trial and has completed Phase 1 evaluation in subjects with plaque psoriasis (NCT02193815), although this was only a 12 day study. | View clinical data
Bioactivity Comments: In vitro and in vivo potencies, and the pharmacokinetic and safety profiles of PF-06263276 indicate suitability for inhaled or topical therapy to treat inflammatory diseases, such as COPD or psoriasis, through direct administration to the lungs or skin, thus avoiding any systemic effects of JAK inhibition [27]. IC50 evaluation was performed at 100nM ATP. | View biological activity
GSK2982772
Immuno Disease Comments: Clinical candidate in psoriasis.
Clinical Use: GSK2982772 is in Phase 2 clinical trials in psoriasis (NCT02776033), rheumatoid arthritis (NCT02858492), and ulcerative colitis (NCT02903966). | View clinical data
Bioactivity Comments: In a screening panel 10μM GSK2982772 did not inhibit any of the 339 kinases tested by >50% (a level assessed as being inactive). GSK2982772 prevented TNF-induced necrotic cell death, and was effective in an ulcerative colitis explant assay for blocking spontaneous cytokine release [21]. | View biological activity
KD025
Immuno Disease Comments: Phase 2 clinical candidate for moderate to severe plaque psoriasis (NCT02852967).
Clinical Use: KD025 is in Phase 2 clinical trials evaluating its anti-inflammatory and anti-fibrotic activity. | View clinical data
metformin
Immuno Disease Comments: Clinical trial NCT02644954 was designed to test for efficacy of adjunct metformin in patients with moderate chronic plaque psoriasis, however it is unclear if this trial was ever initiated.
Clinical Use: Used in the management of non-insulin dependent type 2 diabetes as an adjunct to diet and exercise. Also used in the management of polycystic ovary syndrome (PCOS).
Metformin is combined with in Invokamet®, (also marketed as Vokanamet®) the first fixed-dose combination of an SGLT2 inhibitor with metformin to be approved (by the US FDA, 2014). Later in 2014, the US FDA approved a second SGLT2/metformin drug, Xigduo XR®, which contains (as dapagliflozin propanediol monohydrate PubChem CID 56841155) and metformin hydrochloride. The first approval of a metformin-containing drug mixture by the EMA was for Avandamet (rosiglitazone plus metformin), although this drug was later withdrawn from the market. Avandamet has been superceeded by newer and more effective anti-diabetes combination drugs. | View clinical data
Bioactivity Comments: As the molecular mechanism of metformin is incompletely understood we have not tagged a primary drug target. | View biological activity
galectin-3
Immuno Disease Comments: Experiments in mouse models shows that galectin 3 deficiency contributes to the development of psoriasis-like inflammatory skin lesions. Notably galectin 3 expression is down-regulated in lesional skin from psoriasis patients, but not in their non-lesional skin.
certolizumab pegol
Immuno Disease Comments: Approved drug for moderate-to-severe plaque psoriasis (FDA 2018) and psoriatic arthritis (EMA 2009).
Clinical Use: Used to treat rheumatoid arthritis (RA) and Crohn's disease [7]. May also have some effect in related conditions such as axial spondyloarthritis [51]. The EMA granted Europe-wide approval for the use of this drug in patients with RA (moderate to severe, active disease and severe, active and progressive disease), axial spondyloarthritis and psoriatic arthritis in 2009. FDA approval was expanded to include treatment of moderate-to-severe plaque psoriasis, in June 2018. | View clinical data
Bioactivity Comments: Certolizumab pegol neutralises soluble TNFα in vitro, with an IC90 of 3ng/ml [42], neutralises the effects mediated by membrane bound TNFα, and inhibits production of IL-1β in monocytes stimulated with LPS. | View biological activity
AbGn-168H
Immuno Disease Comments: Phase 2 clinical evaluation of AbGn-168H in patients with moderate to severe chronic plaque psoriasis (NCT01855880) and active psoriatic arthritis (NCT02267642) has been completed, but results have not yet been published (July 2018).
Clinical Use: AbGn-168H has completed Phase 2 clinical evaluation in patients with moderate to severe chronic plaque psoriasis (NCT01855880) and active psoriatic arthritis (NCT02267642). A Phase 2 study in patients with moderate to severe active, anti-TNFα and/or anti-integrin refractory ulcerative colitis has been initiated (NCT03298022), as has a Phase 1 study for steroid-refractory acute graft-versus-host disease (GvHD; NCT03327857). FDA orphan drug designation for the treatment of acute GvHD was granted in January 2018 [12]. | View clinical data

References

Show »

1. Akama T, Baker SJ, Zhang YK, Hernandez V, Zhou H, Sanders V, Freund Y, Kimura R, Maples KR, Plattner JJ. (2009) Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis. Bioorg. Med. Chem. Lett., 19 (8): 2129-32. [PMID:19303290]

2. Baeten D, Sieper J, Braun J, Baraliakos X, Dougados M, Emery P, Deodhar A, Porter B, Martin R, Andersson M et al.. (2015) Secukinumab, an Interleukin-17A Inhibitor, in Ankylosing Spondylitis. New England Journal od Medicine, 373 (26): 2534-2548.

3. Beidler CB, Bright SW, Girard DS, Kikly KK. (2015) Antibodies that bind to IL-23. Patent number: US9023358B2. Assignee: Eli Lilly and Co Ltd (GB). Priority date: 08/03/2013. Publication date: 05/05/2015.

4. Benson J, Carton J, Mark Cunningham M, Orlovsky YI, Rauchenberger R, Sweet R. (2011) Human anti-IL-23 antibodies, compositions, methods and uses. Patent number: US7935344. Assignee: Centocor Ortho Biotech Inc.. Priority date: 29/12/2005. Publication date: 01/05/2011.

5. Bergh K, Iversen OJ, Lysvand H. (1993) Surprisingly high levels of anaphylatoxin C5a des Arg are extractable from psoriatic scales. Arch. Dermatol. Res., 285 (3): 131-4. [PMID:8503693]

6. Bissonnette R, Bolduc C, Maari C, Nigen S, Webster JM, Tang L, Lyle M. (2012) Efficacy and safety of topical WBI-1001 in patients with mild to moderate psoriasis: results from a randomized double-blind placebo-controlled, phase II trial. J Eur Acad Dermatol Venereol, 26 (12): 1516-21. [PMID:22077962]

7. Choy EH, Hazleman B, Smith M, Moss K, Lisi L, Scott DG, Patel J, Sopwith M, Isenberg DA. (2002) Efficacy of a novel PEGylated humanized anti-TNF fragment (CDP870) in patients with rheumatoid arthritis: a phase II double-blinded, randomized, dose-escalating trial. Rheumatology (Oxford), 41 (10): 1133-7. [PMID:12364632]

8. David M, Akerman L, Ziv M, Kadurina M, Gospodinov D, Pavlotsky F, Yankova R, Kouzeva V, Ramon M, Silverman MH et al.. (2012) Treatment of plaque-type psoriasis with oral CF101: data from an exploratory randomized phase 2 clinical trial. J Eur Acad Dermatol Venereol, 26 (3): 361-7. [PMID:21504485]

9. Dogra S, D S K, Budamakuntla L, Srinivas CR, Khopkar U, Gupta S, Shetty N, Pratap DV, Gopal MG, Rao TN et al.. (2015) Long-term efficacy and safety of itolizumab in patients with moderate-to-severe chronic plaque psoriasis: A double-blind, randomized-withdrawal, placebo-controlled study. J. Am. Acad. Dermatol., 73 (2): 331-3.e1. [PMID:26183983]

10. Elain G, Jeanneau K, Rutkowska A, Mir AK, Dev KK. (2014) The selective anti-IL17A monoclonal antibody secukinumab (AIN457) attenuates IL17A-induced levels of IL6 in human astrocytes. Glia, 62 (5): 725-35. [PMID:24677511]

11. Farahnik B, Beroukhim K, Zhu TH, Abrouk M, Nakamura M, Singh R, Lee K, Bhutani T, Koo J. (2016) Ixekizumab for the Treatment of Psoriasis: A Review of Phase III Trials. Dermatol Ther (Heidelb), 6 (1): 25-37. [PMID:26910853]

12. FDA. neihulizumab. Accessed on 02/07/2018. Modified on 02/07/2018. US FDA: Orphan Drug Designations and Approvals, https://www.accessdata.fda.gov/scripts/opdlisting/oopd/detailedIndex.cfm?cfgridkey=622617

13. Fishman P, Cohen S, Bar-Yehuda S. (2013) Targeting the A3 adenosine receptor for glaucoma treatment (review). Mol Med Rep, 7 (6): 1723-5. [PMID:23563604]

14. Fouser LA, Hegen M, Luxenberg DP, O'Toole M. (2010) Methods of using antibodies against human IL-22. Patent number: US7811567. Assignee: Wyeth Llc. Priority date: 21/02/2006. Publication date: 12/10/2010.

15. Genovese MC, Greenwald M, Cho CS, Berman A, Jin L, Cameron GS, Benichou O, Xie L, Braun D, Berclaz PY et al.. (2014) A phase II randomized study of subcutaneous ixekizumab, an anti-interleukin-17 monoclonal antibody, in rheumatoid arthritis patients who were naive to biologic agents or had an inadequate response to tumor necrosis factor inhibitors. Arthritis Rheumatol, 66 (7): 1693-704. [PMID:24623718]

16. Giles-Komar J, Knight DM, Peritt D, Scallon B, Shealy D. (2005) Also an IL-12 anti-idiotype antibody to the antibody. Patent number: US6902734. Assignee: Centocor, Inc.. Priority date: 07/08/2000. Publication date: 07/06/2005.

17. Gordon KB, Blauvelt AB, Papp KA, Langley RG, Luger T, Ohtsuki M, Reich K, Amato D, Ball SG, Braun DK et al.. (2016) Phase 3 Trials of Ixekizumab in Moderate-to-Severe Plaque Psoriasis. New England Journal of Medicine, Online first.

18. Goto M, Chow J, Muramoto K, Chiba K, Yamamoto S, Fujita M, Obaishi H, Tai K, Mizui Y, Tanaka I et al.. (2009) E6201 [(3S,4R,5Z,8S,9S,11E)-14-(ethylamino)-8, 9,16-trihydroxy-3,4-dimethyl-3,4,9,19-tetrahydro-1H-2-benzoxacyclotetradecine-1,7(8H)-dione], a novel kinase inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase (MEK)-1 and MEK kinase-1: in vitro characterization of its anti-inflammatory and antihyperproliferative activities. J. Pharmacol. Exp. Ther., 331 (2): 485-95. [PMID:19684251]

19. Guay D, Boulet L, Friesen RW, Girard M, Hamel P, Huang Z, Laliberté F, Laliberté S, Mancini JA, Muise E et al.. (2008) Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor. Bioorg. Med. Chem. Lett., 18 (20): 5554-8. [PMID:18835163]

20. Gupta AK, Chow M. (2004) A review of prednicarbate (Dermatop). Skin Therapy Lett., 9 (10): 5-6, 9. [PMID:15657633]

21. Harris PA, Berger SB, Jeong JU, Nagilla R, Bandyopadhyay D, Campobasso N, Capriotti CA, Cox JA, Dare L, Dong X et al.. (2017) Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases. J. Med. Chem., 60 (4): 1247-1261. [PMID:28151659]

22. Helmer E, Watling M, Jones E, Tytgat D, Jones M, Allen R, Payne A, Koch A, Healy E. (2017) First-in-human studies of seletalisib, an orally bioavailable small-molecule PI3Kδ inhibitor for the treatment of immune and inflammatory diseases. Eur. J. Clin. Pharmacol., 73 (5): 581-591. [PMID:28160012]

23. Jaffe GJ, Dick AD, Brézin AP, Nguyen QD, Thorne JE, Kestelyn P, Barisani-Asenbauer T, Franco P, Heiligenhaus A, Scales D et al.. (2016) Adalimumab in Patients with Active Noninfectious Uveitis. N. Engl. J. Med., 375 (10): 932-43. [PMID:27602665]

24. Jardieu PM, Presta LG. (2004) Method of treatment using humanized anti-CD11a antibodies. Patent number: US6703018. Assignee: Genentech, Inc.. Priority date: 27/11/1996. Publication date: 19/03/2004.

25. Jayaraman K. (2013) Biocon's first-in-class anti-CD6 mAb reaches the market. Nat. Biotechnol., 31 (12): 1062-3. [PMID:24316625]

26. Johansen C, Rittig AH, Mose M, Bertelsen T, Weimar I, Nielsen J, Andersen T, Rasmussen TK, Deleuran B, Iversen L. (2017) STAT2 is involved in the pathogenesis of psoriasis by promoting CXCL11 and CCL5 production by keratinocytes. PLoS ONE, 12 (5): e0176994. [PMID:28472186]

27. Jones P, Storer RI, Sabnis YA, Wakenhut FM, Whitlock GA, England KS, Mukaiyama T, Dehnhardt CM, Coe JW, Kortum SW et al.. (2017) Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin. J. Med. Chem., 60 (2): 767-786. [PMID:27983835]

28. Kay J, Matteson EL, Dasgupta B, Nash P, Durez P, Hall S, Hsia EC, Han J, Wagner C, Xu Z et al.. (2008) Golimumab in patients with active rheumatoid arthritis despite treatment with methotrexate: a randomized, double-blind, placebo-controlled, dose-ranging study. Arthritis Rheum., 58 (4): 964-75. [PMID:18383539]

29. Kerscher MJ, Korting HC. (1992) Topical glucocorticoids of the non-fluorinated double-ester type. Lack of atrophogenicity in normal skin as assessed by high-frequency ultrasound. Acta Derm. Venereol., 72 (3): 214-6. [PMID:1357864]

30. Kiuchi M, Marukawa K, Kobayashi N, Sugahara K. (2009) Amine Compound and Use Thereof for Medical Purposes. Patent number: US20090137530. Assignee: Mitsubishi Tanabe Pharma Corporation. Priority date: 15/12/2005. Publication date: 28/05/2009.

31. Kogan TP, Dupré B, Bui H, McAbee KL, Kassir JM, Scott IL, Hu X, Vanderslice P, Beck PJ, Dixon RA. (1998) Novel synthetic inhibitors of selectin-mediated cell adhesion: synthesis of 1,6-bis[3-(3-carboxymethylphenyl)-4-(2-alpha-D- mannopyranosyloxy)phenyl]hexane (TBC1269). J. Med. Chem., 41 (7): 1099-111. [PMID:9544210]

32. Korting HC, Vieluf D, Kerscher M. (1992) 0.25% prednicarbate cream and the corresponding vehicle induce less skin atrophy than 0.1% betamethasone-17-valerate cream and 0.05% clobetasol-17-propionate cream. Eur. J. Clin. Pharmacol., 42 (2): 159-61. [PMID:1618247]

33. Krueger JG, Ferris LK, Menter A, Wagner F, White A, Visvanathan S, Lalovic B, Aslanyan S, Wang EE, Hall D et al.. (2015) Anti-IL-23A mAb BI 655066 for treatment of moderate-to-severe psoriasis: Safety, efficacy, pharmacokinetics, and biomarker results of a single-rising-dose, randomized, double-blind, placebo-controlled trial. J. Allergy Clin. Immunol., 136 (1): 116-124.e7. [PMID:25769911]

34. Krupashankar DS, Dogra S, Kura M, Saraswat A, Budamakuntla L, Sumathy TK, Shah R, Gopal MG, Narayana Rao T, Srinivas CR et al.. (2014) Efficacy and safety of itolizumab, a novel anti-CD6 monoclonal antibody, in patients with moderate to severe chronic plaque psoriasis: results of a double-blind, randomized, placebo-controlled, phase-III study. J. Am. Acad. Dermatol., 71 (3): 484-92. [PMID:24703722]

35. McInnes IB, Mease PJ, Kirkham B, Kavanaugh A, Ritchlin CT, Rahman P, van der Heijde D, Landewé R, Conaghan PG, Gottlieb AB et al.. (2015) Secukinumab, a human anti-interleukin-17A monoclonal antibody, in patients with psoriatic arthritis (FUTURE 2): a randomised, double-blind, placebo-controlled, phase 3 trial. Lancet, 386 (9999): 1137-46. [PMID:26135703]

36. Mease PJ, Genovese MC, Greenwald MW, Ritchlin CT, Beaulieu AD, Deodhar A, Newmark R, Feng J, Erondu N, Nirula A. (2014) Brodalumab, an Anti-IL17RA Monoclonal Antibody, in Psoriatic Arthritis. N. Engl. J. Med., 370 (24): 2295-2306. [PMID:24918373]

37. Mease PJ, McInnes IB, Kirkham B, Kavanaugh A, Rahman P, van der Heijde D, Landewé R, Nash P, Pricop L, Yuan J et al.. (2015) Secukinumab Inhibition of Interleukin-17A in Patients with Psoriatic Arthritis. N. Engl. J. Med., 373 (14): 1329-39. [PMID:26422723]

38. Miller GT, Hochman PS, Meier W, Tizard R, Bixler SA, Rosa MD, Wallner BP. (1993) Specific interaction of lymphocyte function-associated antigen 3 with CD2 can inhibit T cell responses. J. Exp. Med., 178 (1): 211-22. [PMID:7686212]

39. Moffett K, Konteatis Z, Nguyen D, Shetty R, Ludington J, Fujimoto T, Lee KJ, Chai X, Namboodiri H, Karpusas M et al.. (2011) Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). Bioorg. Med. Chem. Lett., 21 (23): 7155-65. [PMID:22014550]

40. Mrowietz U, Koch WA, Zhu K, Wiedow O, Bartels J, Christophers E, Schröder JM. (2001) Psoriasis scales contain C5a as the predominant chemotaxin for monocyte-derived dendritic cells. Exp. Dermatol., 10 (4): 238-45. [PMID:11493312]

41. Muramoto K, Goto M, Inoue Y, Ishii N, Chiba K, Kuboi Y, Omae T, Wang YJ, Gusovsky F, Shirota H. (2010) E6201, a novel kinase inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase-1 and mitogen-activated protein kinase/extracellular signal-regulated kinase kinase kinase-1: in vivo effects on cutaneous inflammatory responses by topical administration. J. Pharmacol. Exp. Ther., 335 (1): 23-31. [PMID:20627998]

42. Nesbitt A, Fossati G, Bergin M, Stephens P, Stephens S, Foulkes R, Brown D, Robinson M, Bourne T. (2007) Mechanism of action of certolizumab pegol (CDP870): in vitro comparison with other anti-tumor necrosis factor alpha agents. Inflamm. Bowel Dis., 13 (11): 1323-32. [PMID:17636564]

43. Ott GR, Cheng M, Learn KS, Wagner J, Gingrich DE, Lisko JG, Curry M, Mesaros EF, Ghose AK, Quail MR et al.. (2016) Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK). J. Med. Chem., 59 (16): 7478-96. [PMID:27527804]

44. Pargellis C, Tong L, Churchill L, Cirillo PF, Gilmore T, Graham AG, Grob PM, Hickey ER, Moss N, Pav S et al.. (2002) Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site. Nat. Struct. Biol., 9 (4): 268-72. [PMID:11896401]

45. Reich K, Papp KA, Blauvelt A, Tyring SK, Sinclair R, Thaçi D, Nograles K, Mehta A, Cichanowitz N, Li Q et al.. (2017) Tildrakizumab versus placebo or etanercept for chronic plaque psoriasis (reSURFACE 1 and reSURFACE 2): results from two randomised controlled, phase 3 trials. Lancet, 390 (10091): 276-288. [PMID:28596043]

46. Rodriguez PC, Torres-Moya R, Reyes G, Molinero C, Prada D, Lopez AM, Hernandez IM, Hernandez MV, Martinez JP, Hernandez X et al.. (2012) A clinical exploratory study with itolizumab, an anti-CD6 monoclonal antibody, in patients with rheumatoid arthritis. Results Immunol, 2: 204-11. [PMID:24371585]

47. Shen Y, Boivin R, Yoneda N, Du H, Schiller S, Matsushima T, Goto M, Shirota H, Gusovsky F, Lemelin C et al.. (2010) Discovery of anti-inflammatory clinical candidate E6201, inspired from resorcylic lactone LL-Z1640-2, III. Bioorg. Med. Chem. Lett., 20 (10): 3155-7. [PMID:20399648]

48. Smith SH, Jayawickreme C, Rickard DJ, Nicodeme E, Bui T, Simmons C, Coquery CM, Neil J, Pryor WM, Mayhew D et al.. (2017) Tapinarof Is a Natural AhR Agonist that Resolves Skin Inflammation in Mice and Humans. J. Invest. Dermatol., 137 (10): 2110-2119. [PMID:28595996]

49. Smith SH, Peredo CE, Takeda Y, Bui T, Neil J, Rickard D, Millerman E, Therrien JP, Nicodeme E, Brusq JM et al.. (2016) Development of a Topical Treatment for Psoriasis Targeting RORγ: From Bench to Skin. PLoS ONE, 11 (2): e0147979. [PMID:26870941]

50. Sofen H, Smith S, Matheson RT, Leonardi CL, Calderon C, Brodmerkel C, Li K, Campbell K, Marciniak Jr SJ, Wasfi Y et al.. (2014) Guselkumab (an IL-23-specific mAb) demonstrates clinical and molecular response in patients with moderate-to-severe psoriasis. J. Allergy Clin. Immunol., 133 (4): 1032-40. [PMID:24679469]

51. Song IH, Rudwaleit M. (2013) Certolizumab pegol in axial spondyloarthritis. Expert Rev Clin Immunol, 9 (12): 1161-72. [PMID:24215406]

52. Sugahara K, Maeda Y, Shimano K, Mogami A, Kataoka H, Ogawa K, Hikida K, Kumagai H, Asayama M, Yamamoto T et al.. (2017) Amiselimod, a novel sphingosine 1-phosphate receptor-1 modulator, has potent therapeutic efficacy for autoimmune diseases, with low bradycardia risk. Br. J. Pharmacol., 174 (1): 15-27. [PMID:27714763]

53. Thurmond RL, Greenspan A, Radziszewski W, Xu XL, Miao Y, Chen B, Ge T, Zhou B, Baker DG, Pavlova D et al.. (2016) Toreforant, A Histamine H4 Receptor Antagonist, in Patients with Active Rheumatoid Arthritis Despite Methotrexate Therapy: Results of 2 Phase II Studies. J. Rheumatol., 43 (9): 1637-42. [PMID:27422891]

54. Tocker J, Mehlin C, Lim AC. (2010) Neutralizing determinants of IL-17 Receptor A and antibodies that bind thereto. Patent number: US7767206. Assignee: Amgen Inc.. Priority date: 02/10/2006. Publication date: 03/08/2010.

55. Towne JE, Cheng JD, O'neill JC, Zhang Y, Sun Y, Cerne H, Piper DE, Ketcherm RR. (2011) Human il-23 antigen binding proteins. Patent number: WO2011056600. Assignee: Amgen Inc.. Priority date: 26/10/2009. Publication date: 12/05/2011.

56. Varani K, Padovan M, Govoni M, Vincenzi F, Trotta F, Borea PA. (2010) The role of adenosine receptors in rheumatoid arthritis. Autoimmun Rev, 10 (2): 61-4. [PMID:20691813]

57. Watz H, Bock D, Meyer M, Schierhorn K, Vollhardt K, Woischwill C, Pedersen F, Kirsten A, Beeh KM, Meyer-Sabellek W et al.. (2013) Inhaled pan-selectin antagonist Bimosiamose attenuates airway inflammation in COPD. Pulm Pharmacol Ther, 26 (2): 265-70. [PMID:23257347]

58. Zhou H, Jang H, Fleischmann RM, Bouman-Thio E, Xu Z, Marini JC, Pendley C, Jiao Q, Shankar G, Marciniak SJ et al.. (2007) Pharmacokinetics and safety of golimumab, a fully human anti-TNF-alpha monoclonal antibody, in subjects with rheumatoid arthritis. J Clin Pharmacol, 47 (3): 383-96. [PMID:17322150]