Alvespimycin is a derivative of geldanamycin and heat shock protein (HSP) 90 inhibitor. It has been used in trials studying the treatment of solid tumor in various cancer as an... In comparison to the first HSP90 inhibitor tanespimycin, it exhibits some pharmacologically desirable properties such as reduced metabolic liability, lower plasma protein binding, increased water solubility, higher oral bioavailability, reduced hepatotoxicity and superior antitumor activity.
- Mechanism
- Curator reviewed · 1 reference
Alvespimycin inhibits HSP90 and its regulation of correct folding and function of many cellular signalling proteins, which are referred to as Hsp90 client proteins. These client proteins are also referred to as oncoproteins and include Her-2, EGFR, Akt, Raf-1, p53, Bcr-Abl, Cdk4, Cdk6 and steroid receptors that are involved in cellular signalling pathways that drive cellular proliferation and counteract apoptosis. They are often over-expressed or mutated in tumors, and contribute to cancer progression and therapy resistance [A19244 ]. Alvespimycin promotes an anticancer activity by disrupting Hsp90's chaperone function and inducing the proteasomal degradation of oncoproteins. It is shown to reduce the levels of CDK4 and ERBB2.
- Primary indication
- Investigated for use as an antineoplastic agent for solid tumors, advanced solid tumours or acute myeloid leukaemia.Curator reviewed
- Formula / weight
- C32H48N4O8 · 616.7455 g/mol (avg)
- Also known as
- 17-DMAG · DMAG
- Code names
- KOS-1022 · NSC-707545
Resolves to
KUFRQPKVAWMTJO-LMZWQJSESA-NSMILESCO[C@H]1C[C@H](C)CC2=C(NCCN(C)C)C(=O)C=C(NC(=O)\C(C)=C\C=C/[C@H](OC)[C@@H](OC(N)=O)\C(C)=C\[C@H](C)[C@H]1O)C2=OWhat you can answer from here — as of September 13, 2026
Which drugs share a target with Alvespimycin, and which of those have an active Phase 3 trial?
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