Preferred Label : Nendratareotide Uzatansine;
NCIt synonyms : SSTR2-targeting Protein/DM1 Conjugate PEN-221;
NCIt definition : A miniaturized drug conjugate composed of a peptide analog of somatostatin that targets
the somatostatin receptor 2 (SSTR2) and is conjugated, through a cleavable linker,
to the microtubule-binding cytotoxic maytansinoid DM1 (mertansine), with potential
anti-tumor activity. Upon administration, the peptide ligand moiety of nendratareotide
uzatansine targets and binds to SSTR2, which is overexpressed on certain tumor cell
types. Binding stimulates SSTR2-mediated endocytosis of the agent; upon internalization,
the DM1 moiety is released and binds to tubulin, thereby disrupting microtubule assembly/disassembly
dynamics. This inhibits both cell division and the proliferation of SSTR2-expressing
cancer cells. Compared to antibody-drug conjugates (ADCs), miniaturized drug conjugates
are much smaller and can more easily penetrate and distribute in dense tumor tissue.;
UNII : L8993M383E;
CAS number : 1853254-97-3;
Molecule name : PEN-221; SSTR2PEN-221; PEN 221;
NCI Metathesaurus CUI : CL514580;
Origin ID : C131562;
UMLS CUI : C5554539;
Semantic type(s)
- concept_is_in_subset
- has_target
