Preferred Label : AlphaVbeta1/8 Inhibitor PLN-101095;
NCIt synonyms : AlphaVbeta1/AlphaVbeta8 Inhibitor PLN-101095; Integrin Inhibitor PLN-101095; Immunocytokine IGM-7354;
NCIt definition : An orally bioavailable, small molecule dual inhibitor of the integrins alpha V beta
1 (aVb1) and 8 (aVb8), with potential immunomodulating and antineoplastic activities.
Upon oral administration, alphaVbeta1/8 inhibitor PLN-101095 targets, binds to and
inhibits the integrins aVb1 and aVb8 in the tumor microenvironment (TME). This blocks
aVb1/8-mediated signaling and prevents the activation of tumor growth factor-beta
(TGF-b). Inhibition of TGF-b promotes T-cell infiltration and the release of pro-inflammatory
cytokines into the TME, and results in a cytotoxic T-lymphocytes (CTLs)-mediated immune
response against tumor cells. In addition, this may inhibit the TGF-beta-mediated
resistance to checkpoint inhibitors and may sensitize tumors to checkpoint inhibitors.
The integrins aVb1 and aVb8 are overexpressed in a variety of tumor types and play
a key role in the activation and signaling of TGF-b.;
Molecule name : PLN-101095; PLN 101095;
NCI Metathesaurus CUI : CL1926974;
Origin ID : C204745;
UMLS CUI : C5908054;
Semantic type(s)
- concept_is_in_subset
