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AT-101 + topotecan
- Development stage
- Unknown
- Lead developer
- Ascenta Therapeutics
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
**AT-101 + topotecan** is a combination regimen used in clinical trials for the treatment of relapsed and refractory small cell lung cancer (SCLC). **AT-101** is an oral *pan Bcl-2 family protein inhibitor* (BH3 mimetic, gossypol acetic acid derivative) that inhibits anti-apoptotic Bcl-2 proteins (including Bcl-2, Bcl-xL, Bcl-w, Mcl-1), thereby lowering the threshold for apoptosis. **Topotecan** is a topoisomerase I inhibitor and acts as a cytotoxic chemotherapeutic agent. The combination aims to overcome resistance to cell death in SCLC by targeting both DNA topology and apoptosis pathways. Studies show that AT-101 can be safely combined with a reduced dose of topotecan, but response rates did not reach criteria for expansion; most observed toxicities were hematologic[1][3].
- Other names
- AT-101 + topotecan
02
Targets
BCL2L1 (B-cell lymphoma-extra large protein)MCL1 (Myeloid cell leukemia sequence 1)TOP1 (DNA Topoisomerase I)
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