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Also known as OTX105, MK-8628
Birabresib · 1 trial · 6 indications
A DLT was defined as any of the following toxicities that were considered by the investigator to be related to MK-8628: Hematologic toxicity: Grade 4 hematologic toxicity or febrile neutropenia, Grade 3 neutropenia with infection, Grade 3 thrombocytopenia with bleeding or lasting \>7 days; Non-hematologic toxicity: Grade 3 or 4 non-hematologic toxicity (regardless of duration) unless it was not optimally managed with supportive care, Grade 3 or 4 laboratory abnormality, with or without symptoms, lasting \>48 hours, Intolerable Grade 2 non-hematologic toxicity resulting in study drug discontinuation or delay \>7 days with or without dose reduction, Designated alanine aminotransferase (ALT) or aspartate aminotransferase (AST) liver test abnormalities; Treatment delay \>2 weeks or dose reduction requirement for initiating Cycle 2.
| Arm | Type | Description |
|---|---|---|
| Continuous Dosing Regimen | EXPERIMENTAL | Participants receive birabresib capsules once daily in a fasted state in the morning on Days 1-21 of each 21-day cycle. Starting dose for dose escalation is 80 mg. |
| Days 1-7 Dosing Regimen | EXPERIMENTAL | Participants receive birabresib capsules once daily in a fasted state in the morning on Days 1-7 of each 21-day cycle. Starting dose for dose escalation is 100 mg. |
| Name | Type | Description |
|---|---|---|
| Birabresib | DRUG | Birabresib 10, 20 and/or 40 mg oral capsules |
Inclusion Criteria: 1. Signed informed consent obtained prior to initiation of any study-specific procedures and treatment; 2. Histologically or cytologically confirmed diagnosis of one of the following advanced or metastatic solid tumors for which standard therapy either does not exist or has prov...
Birabresib is an investigational small molecule drug being developed by Merck & Company, Inc. (MRK) for the treatment of cancer. It is a BET bromodomain inhibitor that has been studied in adults with selected advanced solid tumors, including NUT midline carcinoma. It remains in clinical development and is not an approved therapy.
Birabresib has been studied as a treatment for NUT midline carcinoma, a rare and aggressive cancer. It was evaluated in a Phase 1 dose-finding study in adults with selected advanced solid tumors, including NUT midline carcinoma, along with triple negative breast cancer, ALK-rearranged or KRAS-mutant non-small cell lung cancer, castrate-resistant prostate cancer, and pancreatic ductal adenocarcinoma.
Birabresib targets the bromodomain and extra-terminal (BET) proteins, specifically BRD2, BRD3, BRD4, and BRDT. It acts as an inhibitor of these proteins. BET proteins are epigenetic readers that influence gene transcription, and inhibiting them is the proposed mechanism of action for birabresib in cancer.
Birabresib is developed by Merck & Company, Inc., which trades under the ticker MRK. The drug is also known by the code MK-8628, and the Phase 1 study of birabresib was conducted under the MK-8628-003 protocol.
Birabresib is in Phase 1 clinical development. It has not been approved by the FDA and remains an investigational agent. The single registered trial of birabresib is a completed Phase 1 dose-finding study, and no active trials of the drug are currently listed.
Birabresib was evaluated in one Phase 1 trial, NCT02259114, titled a dose-finding study of birabresib (MK-8628), a small molecule inhibitor of the BET proteins, in adults with selected advanced solid tumors. That trial is completed and enrolled 47 participants. It was a controlled study with biomarker-selected patients and was not randomized or double-blind.
Yes, birabresib is also known as MK-8628. Merck & Company, Inc. uses the MK-8628 designation for the compound, and the Phase 1 trial of birabresib was conducted under the protocol name MK-8628-003. Both names refer to the same investigational BET inhibitor.