Drug intelligence / Profile preview

AT-101 + docetaxel

Development stage
Unknown
Lead developer
Ascenta Therapeutics
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

AT-101 + docetaxel is a combination therapy under investigation for cancer treatment, particularly non-small cell lung cancer and multiple myeloma. AT-101 is an orally active, small molecule inhibitor of the Bcl‑2 family of anti-apoptotic proteins, including B-cell lymphoma 2 protein (Bcl‑2), B-cell lymphoma-extra large protein (Bcl-xL), Myeloid cell leukemia sequence 1 protein (Mcl‑1), and BCL-w protein (Bcl-w). By inhibiting these proteins, AT‑101 promotes apoptosis in cancer cells via the mitochondrial pathway[5][6]. Docetaxel is a taxane-class chemotherapy agent that binds to microtubules with high affinity and stabilizes them against depolymerization. This disrupts mitotic cell division by preventing microtubule disassembly during metaphase-anaphase transition and leads to apoptosis[4]. The combination has shown synergistic effects in preclinical models and was evaluated in phase 2 clinical trials for advanced or metastatic non-small cell lung cancer[5]. The primary endpoint of improved progression-free survival was not met; however, the regimen was well tolerated.

Brand names
Taxotere (for docetaxel)
Other names
gossypol acetic acid (for AT-101)Docetaxel
02

Targets

Bcl-w (B-cell lymphoma 2-like 2)BCL2L1 (B-cell lymphoma-extra large protein)TUBB (Tubulin (alpha and beta subunits))MCL1 (Myeloid cell leukemia sequence 1)

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