Drug intelligence / Profile preview

AT-101 + docetaxel + 5-fluorouracil

Development stage
Unknown
Lead developer
A28 Therapeutics
Modality
Small Molecules
Administration
Oral (AT-101), Intravenous (docetaxel), Intravenous (5-fluorouracil)
01

Overview

AT-101 + docetaxel + 5-fluorouracil is an experimental combination therapy used in cancer treatment, notably investigated in a Phase I/II trial for patients with locally advanced gastroesophageal carcinoma. **AT-101 (R-(-)-gossypol acetic acid)** is an orally administered, small molecule *BH3 mimetic* that downregulates anti-apoptotic Bcl-2 and related proteins, leading to apoptosis induction via both caspase-dependent and mitochondrial pathways. AT-101 may also suppress angiogenesis and affect pro-angiogenic signaling. **Docetaxel** is a microtubule inhibitor chemotherapy that disrupts cell division, and **5-fluorouracil (5-FU)** is a pyrimidine antimetabolite that inhibits DNA synthesis. The combination aims for enhanced tumor response, as shown by high complete response rates in chemo-radiation protocols in some gastroesophageal cancer patients. Primary mechanisms include enhanced induction of apoptosis, cytotoxicity, and possible cancer stem cell suppression.[1]

Other names
R-(-)-gossypol acetic acid + docetaxel + 5-FU
02

Targets

TUBB (Tubulin (alpha and beta subunits))TS (Thymidylate synthase)GnRHR (Gonadotropin-releasing hormone receptor)

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