Repositioning Candidate Details

Candidate ID: R0919
Source ID: DB06075
Source Type: investigational
Compound Type: small molecule
Compound Name: Linsitinib
Synonyms: Linsitinib
Molecular Formula: C26H23N5O
SMILES: C[C@@]1(O)C[C@@H](C1)C1=NC(=C2N1C=CN=C2N)C1=CC=C2C=CC(=NC2=C1)C1=CC=CC=C1
Structure:
DrugBank Description: An orally bioavailable small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. IGF-1R inhibitor OSI-906 selectively inhibits IGF-1R, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis.
CAS Number: 867160-71-2
Molecular Weight: 421.504
DrugBank Indication: Investigated for use/treatment in cancer/tumors (unspecified) and solid tumors.
DrugBank Pharmacology: In laboratory studies of 28 human tumor cell lines, OSI-906 reduced growth of 15 cell lines representative of colorectal, lung, breast, pancreatic, and pediatric tumors and in mouse models. OSI-906 was particularly effective against tumors that are highly IGF-dependent such as colorectal cancers. According to the researchers, OSI-906 not only slowed tumor growth in mice, but decreased the size of some pre-existing tumors.
DrugBank MoA: IGF-1R stimulates proliferation, enables onogenic transformation, and suppresses apoptosis. Inhibitors of IGF-1R are expected to have broad utility in oncology since the over-expression of IGF-1R and/or its ligands or the down-regulation of ligand binding proteins occurs in numerous human malignancies including lung, colon, breast, prostate, brain and skin cancers. In addition, signaling through the IGF system has been implicated in protecting tumor cells from apoptosis induced by anti-cancer treatments such as cytotoxic agents and EGFR inhibitors.
Targets: Insulin-like growth factor 1 receptor inhibitor; Insulin receptor inhibitor
Inclusion Criteria: Therapeutic strategy associated