tenalisib   Click here for help

GtoPdb Ligand ID: 9907

Synonyms: RP-6530 | RP6530
Immunopharmacology Ligand
Compound class: Synthetic organic
Comment: Tenalisib (RP6530) is an orally active dual PI3K δ/γ inhibitor that is being developed by Rhizen Pharmaceuticals for the potential oral treatment of cancer [4] and inflammation. The chemical structure and its use are claimed in patent US9790224 where it is called Compound A1 [5].
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Ligand Activity Visualisation Charts

These 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.

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View interactive charts of activity data across species

tenalisib is commercially available from our sponsors

2D Structure
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2D Structure

An image of the ligand's 2D structure. For small molecules with SMILES these are drawn using the NCI/CADD Chemical Identifier Resolver. Click on the image to access the chemical structure search tool with the ligand pre-loaded in the structure editor. For other types of ligands, e.g. longer nucleotides and peptides, a manually drawn representation of the molecule may be provided.

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Physico-chemical Properties
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Physico-chemical Properties

Calculated molecular properties are available for small molecules and natural products (not peptides). Properties were generated using the Chemistry Development Kit (CDK) (Willighagen EL et al. Journal of Cheminformatics vol. 9:33. 2017, doi:10.1186/s13321-017-0220-4; https://cdk.github.io/). All properties were selected to enable the prediction of the Lipinski Rule-of-Five profile or ‘druglikeness’ for each ligand. For more info on each category see the help pages.

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Hydrogen bond acceptors 5
Hydrogen bond donors 2
Rotatable bonds 5
Topological polar surface area 96.7
Molecular weight 415.14
XLogP 5.45
No. Lipinski's rules broken 1

Generated using the Chemistry Development Kit (CDK) (Willighagen EL et al. Journal of Cheminformatics vol. 9:33. 2017, doi:10.1186/s13321-017-0220-4; https://cdk.github.io/)
SMILES / InChI / InChIKey
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SMILES / InChI / InChIKey

SMILES (Simplified Molecular Input Line Entry Specification) A specification for unambiguously describing the structure of chemical molecules using short ASCII strings. Canonical SMILES specify a unique representation of the 2D structure without chiral or isotopic specifications. Isomeric SMILES include chiral specification and isotopes.

Standard InChI (IUPAC International Chemical Identifier) and InChIKey InChI is a non-proprietary, standard, textual identifier for chemical substances designed to facilitate linking of information and database searching. An InChIKey is a simplified version of a full InChI, designed for easier web searching.

Generated using the Chemistry Development Kit (CDK) (Willighagen EL et al. Journal of Cheminformatics vol. 9:33. 2017, doi:10.1186/s13321-017-0220-4; https://cdk.github.io/)

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Canonical SMILES CCC(c1oc2ccccc2c(=O)c1c1cccc(c1)F)Nc1ncnc2c1[nH]cn2
Isomeric SMILES CC[C@@H](c1oc2ccccc2c(=O)c1c1cccc(c1)F)Nc1ncnc2c1[nH]cn2
InChI InChI=1S/C23H18FN5O2/c1-2-16(29-23-19-22(26-11-25-19)27-12-28-23)21-18(13-6-5-7-14(24)10-13)20(30)15-8-3-4-9-17(15)31-21/h3-12,16H,2H2,1H3,(H2,25,26,27,28,29)/t16-/m0/s1
InChI Key HDXDQPRPFRKGKZ-INIZCTEOSA-N

Generated using the Chemistry Development Kit (CDK) (Willighagen EL et al. Journal of Cheminformatics vol. 9:33. 2017, doi:10.1186/s13321-017-0220-4; https://cdk.github.io/)
No information available.
Summary of Clinical Use Click here for help
Tenalisib has completed Phase 1 clinical trial as a monotherapy in patients with T cell and B cell lymphomas (NCT02017613), and a Phase 1/2 trial in combination with the PD-1 checkpoint inhibitor pembrolizumab has been initiated in patients with classical Hodgkin lymphoma (NCT03471351). Tenalisib has been granted FDA orphan drug designation [2], and FDA Fast Track designation for the treatment of cutaneous T cell lymphoma (CTCL).
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT03471351 Safety and Efficacy Study of Tenalisib (RP6530) in Combination With Pembrolizumab in Relapsed or Refractory cHL Phase 1 Interventional Rhizen Pharmaceuticals SA
NCT02017613 Safety and Efficacy Study of a Dual PI3K Delta/Gamma Inhibitor in Hematological Malignancies Phase 1 Interventional Rhizen Pharmaceuticals SA Tenalisib demonstrated consistent clinical responses and acceptable safety. 1
NCT02567656 Safety and Efficacy Study of a Dual PI3K Delta/Gamma Inhibitor in T-cell Lymphoma Phase 1 Interventional Rhizen Pharmaceuticals SA Tenalisib demonstrated acceptable safety and promising clinical activity (including 3 complete responses and 13 partial responses out of 35 evaluable patients, with the median duration of response of 4.9 months) in relapsed/refractory peripheral and cutaneous T-cell lymphoma (TCL) 3