Drug intelligence / Profile preview

sta-1474

Development stage
Unknown
Lead developer
Madrigal Pharmaceuticals
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

STA-1474 is a **water-soluble prodrug** that is metabolized into ganetespib (formerly code-named STA-9090), which is a **potent inhibitor of heat shock protein 90 (HSP90)**. HSP90 is a molecular chaperone involved in the stabilization and function of a wide range of client proteins important in tumor cell growth, survival, and resistance to therapy. STA-1474 has shown preclinical antitumor activity in canine tumor cell lines and murine xenograft models, including induction of caspase-dependent apoptosis and downregulation of oncogenic signaling proteins such as pKit/Kit, pMet/Met, pAkt/Akt, and pSTAT3. Phase 1 clinical trials in dogs with spontaneous tumors demonstrated biological activity, including objective responses in malignant mast cell disease, osteosarcoma, melanoma, and thyroid carcinoma. The drug is primarily under investigation as an **antineoplastic targeted therapy** for cancer and has also informed the clinical development of ganetespib in humans[1][3].

Other names
ganetespib prodrug
02

Targets

HSP90 (Heat shock protein 90 chaperone complex)

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