Preferred Label : Albumin-binding Cisplatin Prodrug BTP-114;
NCIt synonyms : Platinum-Prodrug BTP-114; Cisplatin Prodrug BTP-114; Albumin-conjugating Platinum-prodrug BTP-114; Prodrug BTP 114; Cisplatin/Maleimide-based Complex BTP-114;
NCIt definition : A proprietary, albumin-binding platinum (Pt)-based complex containing a prodrug form
of the platinum compound cisplatin and a maleimide moiety, with an ability to strongly
and selectively bind human serum albumin (HSA), and with potential antineoplastic
activity. Upon intravenous administration, the maleimide group of BTP-114 rapidly
conjugates with HSA in the bloodstream; this prolongs the blood circulation, enhances
the half-life, and alters the biodistribution of BTP-114, as compared to cisplatin
alone. Thus, BTP-114 demonstrates enhanced extravasation to the tumor, an increased
accumulation in the tumor tissue and enhanced uptake by cancer cells. The prodrug
form is reduced in the hypoxic tumor cell environment, which releases the highly cytotoxic
active metabolite cisplatin. Once inside the tumor cell, cisplatin binds to nucleophilic
groups, such as GC-rich sites, in DNA and induces intrastrand and interstrand DNA
cross-links, resulting in apoptosis and cell growth inhibition. Compared to cisplatin
alone, BTP-114 has improved selectivity towards tumor tissue, thereby enhancing efficacy
while reducing systemic toxicities.;
Molecule name : BTP-114; BTP 114;
NCI Metathesaurus CUI : CL514482;
Origin ID : C131607;
UMLS CUI : C4329282;
Semantic type(s)
- concept_is_in_subset
