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JNJ-39823277
- Development stage
- Discontinued
- Lead developer
- Johnson & Johnson
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
JNJ-39823277 (also known as TPI 1062) is an orally bioavailable, third-generation taxane derivative originally developed for the treatment of solid tumors. It was discovered by Tapestry Pharmaceuticals and later licensed to Johnson & Johnson. As a microtubule stabilizer, JNJ-39823277 binds to tubulin subunits, promoting microtubule assembly and inhibiting disassembly. This stabilization disrupts the dynamic instability of the mitotic spindle, leading to cell cycle arrest in the G2/M phase and subsequent apoptosis. The compound was specifically designed to overcome multidrug resistance (MDR) mechanisms, such as P-glycoprotein-mediated efflux, which frequently limit the clinical efficacy of first-generation taxanes like paclitaxel. Clinical development reached Phase 1 studies focusing on its safety, tolerability, and pharmacokinetics, including absorption, metabolism, and excretion (AME) profiles in healthy volunteers and cancer patients, before development was discontinued.
- Other names
- TPI 1062TPI1062TPI-1062
02
Targets
TUBB (Tubulin (alpha and beta subunits))
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