Phase 1 dose escalation and expansion of BPC-101 in HR+ breast cancer
Completed phase 1 48/48 enrolledoncology · small molecule
BPC-101 — HR-positive / HER2-negative metastatic breast cancer
An orally available CDK4/6 inhibitor designed for once-daily dosing. The Phase 2 program is enrolling patients who have progressed on a prior CDK4/6 inhibitor plus endocrine therapy.
Investigational candidate. BPC-101 has not been approved by any regulatory authority.
Mechanism of action
How the molecule works.
BPC-101 binds the ATP pocket of CDK4 and CDK6 with high selectivity over CDK1 and CDK2, halting RB phosphorylation and arresting the cell cycle in G1.
Milestones
Program timeline.
- 2021 Candidate nominated done
- 2022 Phase 1 first-patient-in done
- 2023 Phase 1 dose expansion complete done
- 2024 Phase 2 enrollment begins done
- 2025 Phase 2 interim analysis current
- 2026 Phase 2 topline data planned
Clinical trials
2 trials for BPC-101.
Phase 2 study of BPC-101 after prior CDK4/6 inhibition
Recruiting phase 2 180/240 enrolledPublications
4 related publications.
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Structure-based design of a once-daily CDK4/6 inhibitor with selectivity over CDK1 and CDK2
The BPC-101 discovery program: crystallography-guided optimization yielding a selective CDK4/6 inhibitor suitable for once-daily oral dosing.
DOI: 10.1021/acs.jmedchem.[sample] -
Phase 1 dose escalation of BPC-101 in HR+ breast cancer: safety and recommended Phase 2 dose
First-in-human results from the BPC-101 monotherapy and combination expansion cohort in HR+/HER2- metastatic breast cancer.
DOI: 10.1200/JCO.[sample] -
A structure-guided platform for the discovery of selective kinase inhibitors
An overview of the structure-guided discovery platform underlying the BPC-101 and BPC-305 programs.
DOI: 10.1016/j.chembiol.[sample] -
Antibody and antibody-drug conjugate discovery using engineered Fc libraries
Description of the Fc engineering library used to discover BPC-203 and to assemble the BPC-402 linker-payload.
DOI: 10.1073/pnas.[sample]