alphaVbeta1/8 inhibitor PLN-101095

{
  "id": "MLC-T-ONC-009994",
  "term": "alphaVbeta1/8 inhibitor PLN-101095",
  "field": "Oncology and biomedicine",
  "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.",
  "synonyms": [
    "alphaVbeta1/alphaVbeta8 inhibitor PLN-101095",
    "immunocytokine IGM-7354",
    "integrin inhibitor PLN-101095"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/alphavbeta1-8-inhibitor-pln-101095/"
}