Synonyms: AZD-2624 | AZD4901 | MLE4901
Compound class:
Synthetic organic
Comment: Pavinetant (AZD2624) is an orally active antagonist of neurokinin receptor 3 (TACR3) developed initially by AstraZeneca as a potential therapeutic for schizophrenia. This compound was included in AstaZeneca's Open Innovation Pharmacology Toolbox (but has since been removed). Later renamed to AZD4901 it was acquired by Millendo Therapeutics who gave it a new research code of MLE4901 for their development programs for polycystic ovary syndrome and menopausal hot flushes. A successful Phase 2 study for the latter indication was reported in April 2017 [5]. A total of eight analogues are disclosed in the AstraZeneca composition of matter filing [6],
![]() Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
|
References |
1. AstraZeneca.
AZD2624. Accessed on 11/09/2014. Modified on 11/09/2014. astrazeneca.com, http://openinnovation.astrazeneca.com/what-we-offer/compound/azd2624/ |
2. George JT, Kakkar R, Marshall J, Scott ML, Finkelman RD, Ho TW, Veldhuis J, Skorupskaite K, Anderson RA, McIntosh S et al.. (2016)
Neurokinin B Receptor Antagonism in Women With Polycystic Ovary Syndrome: A Randomized, Placebo-Controlled Trial. J Clin Endocrinol Metab, 101 (11): 4313-4321. [PMID:27459523] |
3. Litman RE, Smith MA, Desai DG, Simpson T, Sweitzer D, Kanes SJ. (2014)
The selective neurokinin 3 antagonist AZD2624 does not improve symptoms or cognition in schizophrenia: a proof-of-principle study. J Clin Psychopharmacol, 34 (2): 199-204. [PMID:24525659] |
4. Prague JK, Roberts RE, Comninos AN, Clarke S, Jayasena CN, Mohideen P, Lin VH, Stern TP, Panay N, Hunter MS et al.. (2018)
Neurokinin 3 receptor antagonism rapidly improves vasomotor symptoms with sustained duration of action. Menopause, 25 (8): 862-869. [PMID:29533369] |
5. Prague JK, Roberts RE, Comninos AN, Clarke S, Jayasena CN, Nash Z, Doyle C, Papadopoulou DA, Bloom SR, Mohideen P et al.. (2017)
Neurokinin 3 receptor antagonism as a novel treatment for menopausal hot flushes: a phase 2, randomised, double-blind, placebo-controlled trial. Lancet, 389 (10081): 1809-1820. [PMID:28385352] |
6. Simpson T et al.. (2007)
Alkylsulphonamide quinolines. Patent number: WO2007069977. Assignee: AstraZeneca. Priority date: 12/12/2005. Publication date: 11/12/2006. |