Drug intelligence / Profile preview

obatoclax + bortezomib

Development stage
Phase 2
Lead developer
Teva Pharmaceutical Industries
Modality
Small Molecules
Administration
Intravenous
01

Overview

Obatoclax + bortezomib is a combination of two investigational anticancer drugs tested primarily for hematologic malignancies and some solid tumors. **Obatoclax** is a pan-BCL-2 family inhibitor (specifically, a BH3 mimetic) that targets anti-apoptotic proteins in the BCL-2 family (including BCL-2, BCL-XL, and MCL-1), promoting apoptosis in cancer cells. **Bortezomib** is a small molecule proteasome inhibitor that blocks the 26S proteasome, leading to disrupted proteostasis, increased pro-apoptotic stress, and apoptosis, especially in tumor cells. The combination was investigated based on preclinical synergy, particularly in mantle cell lymphoma and small cell lung cancer models, attributed to overcoming MCL-1–mediated resistance. Clinical trials have shown the combination to be feasible and tolerable, although the synergy observed preclinically was not clearly confirmed in later-stage human studies[1][2][3][5].

Other names
obatoclax mesylateBTZ
02

Targets

26S proteasomeBcl-w (B-cell lymphoma 2-like 2)BCL2L1 (B-cell lymphoma-extra large protein)MCL1 (Myeloid cell leukemia sequence 1)

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