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r-(-)-gossypol acetic acid
- Development stage
- Phase 3
- Lead developer
- Ascenta Therapeutics
- Modality
- Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
**r-(-)-gossypol acetic acid** is the orally bioavailable solvate of the R-enantiomer of gossypol and acetic acid, known for its potential antineoplastic activity. It acts as a natural BH3 mimetic, binding to anti-apoptotic Bcl-2 family proteins including Bcl-2, Bcl-xL, and Mcl-1 with high affinity. By inhibiting these proteins, it induces apoptosis in cancer cells and can also trigger autophagy. r-(-)-gossypol acetic acid has been investigated in Phase I/II clinical trials for advanced solid tumors and shows enhanced effectiveness when combined with other therapies such as androgen deprivation or TRAIL-induced apoptosis[1][4][5][6]. The compound is more potent than the racemic or S-enantiomer forms in inhibiting cell growth and inducing apoptosis[6].
- Other names
- (R)-(-)-Gossypol acetic acidgossypol acetic acid clathrate(R)-Gossypol acetic acid saltU9GNI6VT5NU-9GNI6VT5NU 9GNI6VT5N
02
Targets
BCL2L1 (B-cell lymphoma-extra large protein)MCL1 (Myeloid cell leukemia sequence 1)
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