Preferred Label : Mipsagargin;
NCIt definition : A soluble, thapsigargin prodrug containing the cytotoxic analog of thapsigargin, 8-O-(12Aminododecanoyl)-8-O
debutanoylthapsigargin (12-ADT) linked, via a carboxyl group, to the targeting peptide
containing aspartic acid with potential antineoplastic activity. Upon intravenous
administration, mipsagargin targets prostate specific membrane antigen (PSMA), a type
II membrane carboxypeptidase, which is overexpressed in prostate cancer cells and
in the neovasculature of most solid tumors but not in normal blood vessels. Mipsagargin
is subsequently converted, through hydrolysis, into the active cytotoxic analog of
thapsigargin 12-ADT-Asp. 12-ADT binds to and blocks the Sarcoplasmic/Endoplasmic Reticulum
Calcium ATPase (SERCA) pump, thereby increasing the concentration of cytosolic calcium
which leads to an induction of apoptosis. By preventing nutrient supply to tumor cells,
G-202 may be able to inhibit tumor growth. Compared to thapsigargin alone, thapsigargin
prodrug G-202 is able to achieve higher concentrations of the active agents at the
tumor site while avoiding systemic toxicity.;
UNII : Q032I35QMX;
InChIKey : UPYNTAIBQVNPIH-ODMLWHIESA-N;
CAS number : 1245732-48-2;
Molecule name : G-202;
NCI Metathesaurus CUI : CL416238;
Origin ID : C90554;
UMLS CUI : C4086589;
Semantic type(s)
- concept_is_in_subset
- has_target
