Anti-TROP-2 Antibody-drug Conjugate PF-06664178

**Semantic type:** Pharmacologic Substance

**Definition:** An antibody-drug conjugate (ADC) composed of PF-06478924 (RN926), a humanized immunoglobulin G1 (IgG1) monoclonal antibody targeting the tumor-associated antigen (TAA) trophoblast cell surface protein 2 (trophoblast antigen 2; calcium signal transducer 2; TROP2; TROP-2; TACSTD2; GA733-1; M1S1), site-specifically conjugated via a valine-citrulline cleavable linker with the auristatin-based cytotoxic agent Aur0101 (PF-06380101), with potential antineoplastic activity. Upon administration of anti-TROP-2 ADC PF-06664178, the anti-TROP-2 monoclonal antibody moiety PF-06478924 targets and binds to TROP-2 expressed on tumor cells. Upon binding, internalization and linker cleavage, Aur0101 binds to tubulin and inhibits its polymerization, resulting in G2/M phase arrest and apoptosis of TROP-2-expressing tumor cells. TROP-2 is a transmembrane protein overexpressed in various tumors. Its expression is associated with enhanced tumor aggressiveness, metastasis, drug resistance and increased tumor cell survival.

**Synonyms:** - Anti-TROP-2 ADC PF-06664178 - Anti-TROP-2/Aur0101 ADC PF-06664178 - PF 06664178 - PF-06664178 - PF06664178 - RN 927C - RN-927C - RN927C