NCIt definition : A bispecific ligand drug conjugate targeting both human folate receptor alpha (FR
alpha; FOLR1) and transient receptor potential cation channel subfamily V member 6
(TRPV6; CaT1; CATL) and conjugated to monomethyl auristatin E (MMAE), an auristatin
derivative and potent microtubule disrupting agent, with potential antineoplastic
activity. Upon administration of FR alpha/TRPV6 bispecific ligand drug conjugate CBP-1008,
the bispecific ligand moiety targets and binds to FR alpha and/or TRPV6, which are
overexpressed in certain tumor types. After internalization of the agent, the MMAE
moiety is released and binds to tubulin and inhibits its polymerization, which results
in G2/M phase arrest and apoptosis. This inhibits the proliferation of tumor cells
expressing FR alpha and/or TRPV6. FR alpha is a high-affinity folate-binding protein
and a member of the folate receptor family; it is overexpressed in certain tumor types.
The TRPV6 ion channel plays a key role in calcium homeostasis and is highly selective
for calcium compared to other cations; it is overexpressed in a variety of tumors
and initiates tumor cell growth, proliferation and metastases.;
Semantic type(s)