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Phase Ib Trial With Birabresib, a Small-Molecule Inhibitor of Bromodomain and Extraterminal Proteins, in Patients With Selected Advanced Solid Tumors
Abstract
Purpose: Birabresib (MK-8628/OTX015) is a first-in-class bromodomain inhibitor with activity in select hematologic tumors. Safety, efficacy, and pharmacokinetics of birabresib were evaluated in patients with castrate-resistant prostate cancer, nuclear protein in testis midline carcinoma (NMC), and non–small-cell lung cancer in this phase Ib study. Patients and Methods: Forty-seven patients were enrolled to receive birabresib once daily at starting doses of 80 mg continuously (cohort A) or 100 mg for 7 consecutive days (cohort B) in 21-day cycles using a parallel dose escalation 3 + 3 design. The primary objective was occurrence of dose-limiting toxicities (DLTs) and determination of the recommended phase II dose. Results: Of 46 treated patients, 26 had castrate-resistant prostate cancer, 10 NMC, and 10 non–small-cell lung cancer. For cohort A, four of 19 (21%) evaluable patients had DLTs at 80 mg once daily (grade 3 thrombocytopenia [n = 3], ALT/hyperbilirubinemia [n = 1]) and two of three had DLTs at 100 mg once daily (grade 2 anorexia and nausea with treatment delay > 7 days [n = 1], grade 4 thrombocytopenia [n = 1]). No DLTs occurred in cohort B. Of 46 patients, 38 (83%) had treatment-related adverse events (diarrhea, 17 [37%]; nausea, 17 [37%]; anorexia, 14 [30%]; vomiting, 12 [26%]; thrombocytopenia 10 [22%]). Three patients with NMC (80 mg once daily) had a partial response (Response Evaluation Criteria in Solid Tumors [RECIST] version 1.1) with duration of 1.4 to 8.4 months. Pharmacokinetic analysis indicated a dose-proportional increase in birabresib exposure and rapid absorption. Conclusion: The recommended phase II dose of birabresib in patients with select solid tumors is 80 mg once daily with continuous dosing. Birabresib has dose-proportional exposure and a favorable safety profile, with clinical activity observed in NMC. Future studies of birabresib must consider intermittent scheduling to possibly mitigate the toxicities of chronic dosing.
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Cites
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Targeting bromodomains: epigenetic readers of lysine acetylation
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Cited by
Cohen, E. E. W., Bell, R. B., Bifulco, C. B., Burtness, B., Gillison, M. L., Harrington, K. J., Le, Q.-T., Lee, N. Y., Leidner, R., Lewis, R. L., et al. (2019) · Journal for ImmunoTherapy of Cancer · doi:10.1186/s40425-019-0662-5 · Cited by 722
Epigenetics-targeted drugs: current paradigms and future challenges
Dai, W., Qiao, X., Fang, Y., Guo, R., Bai, P., Liu, S., Li, T., Jiang, Y., Wei, S., Na, Z., et al. (2024) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-024-02039-0 · Cited by 339
Targeting Bromodomain-Selective Inhibitors of BET Proteins in Drug Discovery and Development
Chen, J., Tang, P., Wang, Y., Wang, J., Yang, C., Li, Y., Yang, G., Wu, F., Zhang, J., & Ouyang, L. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c01835 · Cited by 62
The role of protein acetylation in carcinogenesis and targeted drug discovery
Yang, J., Song, C., & Zhan, X. (2022) · Frontiers in Endocrinology · doi:10.3389/fendo.2022.972312 · Cited by 42
Metadata
- Authors
- Lewin, J., Soria, J.-C., Stathis, A., Delord, J.-P., Peters, S., Awada, A., Aftimos, P. G., Bekradda, M., Rezai, K., Zeng, Z., Hussain, A., Perez, S., Siu, L. L., & Massard, C.
- Venue
- Journal of Clinical Oncology
- Published
- 2018-10-20
- Volume
- 36
- Issue
- 30
- Pages
- 3007-3014
- ISSN
- 0732-183X (ISSN-L)
- 1527-7755
- OpenAlex
- W2803008706
- Cited by
- 284
- References
- 25
- FWCI
- 9.02
- Type
- journal article
- Language
- en
- Open access
- closed
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- Lewin, J., Soria, J.-C., Stathis, A., Delord, J.-P., Peters, S., Awada, A., Aftimos, P. G., Bekradda, M., Rezai, K., Zeng, Z., Hussain, A., Perez, S., Siu, L. L., & Massard, C. (2018). Phase Ib Trial With Birabresib, a Small-Molecule Inhibitor of Bromodomain and Extraterminal Proteins, in Patients With Selected Advanced Solid Tumors. Journal of Clinical Oncology. https://doi.org/10.1200/jco.2018.78.2292
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