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linsitinib + bortezomib + dexamethasone
- Development stage
- Unknown
- Lead developer
- Sling Therapeutics
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
A three-drug combination therapy consisting of: - **Linsitinib** (OSI-906/ASP7487): a small molecule inhibitor of the insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR). - **Bortezomib**: a small molecule proteasome inhibitor. - **Dexamethasone**: a synthetic glucocorticoid corticosteroid. This regimen has been investigated in phase 1 trials for relapsed/refractory multiple myeloma. Linsitinib inhibits IGF-1R and IR, thereby blocking growth and survival signaling in tumor cells. Bortezomib inhibits the 26S proteasome, leading to cell cycle arrest and apoptosis in myeloma cells. Dexamethasone acts as an anti-inflammatory and immunosuppressive agent and is standard in myeloma regimens, enhancing the efficacy of other agents. In phase 1 trials, this combination demonstrated manageable toxicity and antimyeloma activity, especially in proteasome inhibitor-refractory patients[1][2][6][8].
- Other names
- linsitinib + bortezomib + dexamethasone
02
Targets
INSR (Insulin receptor)PSMB5 (Proteasome subunit beta Type-5)IGF-1R (Insulin-like growth factor 1 receptor)PSMB9 (Immunoproteasome subunit beta type-1i)GR (Glucocorticoid receptor)
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