birabresib

Ligand id: 8359

Name: birabresib

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 6
Hydrogen bond donors 2
Rotatable bonds 5
Topological polar surface area 120.64
Molecular weight 491.12
XLogP 5.16
No. Lipinski's rules broken 1

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
OTX015 is being used in clinical trials to evaluate the compound's effectiveness against solid tumours and haematological malignancies. Click here to link to ClinicalTrials.gov's complete list of OTX015 trials.
Results from Phase 1 trial in patients with hematological malignancies (NCT01713582) are reported in [2], and pharmacokinetic and dose-escalation results from the same study in [9].
Mechanism Of Action and Pharmacodynamic Effects
The BRDs are important epigenetic regulators of proliferation and differentiation, acting as epigenetic readers. Small molecule BRD inhibitors are being pursued by the pharmaceutical industry as anti-cancer chemotherapeutics [5].[7,11].