Linsitinib

Linsitinib
Clinical data
Other names	OSI-906
Identifiers
	IUPAC name 3-[8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl]-1-methylcyclobutan-1-ol;
CAS Number	867160-71-2;
PubChem CID	11640390;
DrugBank	DB06075;
UNII	15A52GPT8T;
KEGG	D09925;
ChEBI	CHEBI:91402;
ChEMBL	ChEMBL1091644;
CompTox Dashboard (EPA)	DTXSID401007055 ;
Chemical and physical data
Formula	C26H23N5O
Molar mass	421.504 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1(CC(C1)C2=NC(=C3N2C=CN=C3N)C4=CC5=C(C=C4)C=CC(=N5)C6=CC=CC=C6)O;
	InChI InChI=InChI=1S/C26H23N5O/c1-26(32)14-19(15-26)25-30-22(23-24(27)28-11-12-31(23)25)18-8-7-17-9-10-20(29-21(17)13-18)16-5-3-2-4-6-16/h2-13,19,32H,14-15H2,1H3,(H2,27,28); Key:PKCDDUHJAFVJJB-UHFFFAOYSA-N;

Linsitinib is an experimental drug candidate for the treatment of various types of cancer. It is an inhibitor of the insulin receptor and of the insulin-like growth factor 1 receptor (IGF-1R).^[1] This prevents tumor cell proliferation and induces tumor cell apoptosis.^[2]

Linsitinib was granted orphan drug designation for adrenocortical carcinoma in March 2012.^[3]

Phase II clinical trials were initiated for multiple myeloma, ovarian cancer, hepatocellular carcinoma, and NSCLC, but subsatisfactory results caused research for these indications to be discontinued.^[3] A phase III clinical trial found that linsitinib did not increase survival in patients with adrenocortical carcinoma.^[4] As of 2017, no clinical trials were in progress.^[3]

References

↑ Mulvihill MJ, Cooke A, Rosenfeld-Franklin M, Buck E, Foreman K, Landfair D, et al. (September 2009). "Discovery of OSI-906: a selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor". Future Medicinal Chemistry. 1 (6): 1153–1171. doi:10.4155/fmc.09.89. PMID 21425998.
↑ "Linsitinib". Cancer.gov. National Cancer Institute. Retrieved October 16, 2012.
1 2 3 "Linsitinib - Sling Therapeutics". AdisInsight. Springer Nature Switzerland AG.
↑ Fassnacht M, Berruti A, Baudin E, Demeure MJ, Gilbert J, Haak H, et al. (April 2015). "Linsitinib (OSI-906) versus placebo for patients with locally advanced or metastatic adrenocortical carcinoma: a double-blind, randomised, phase 3 study". The Lancet Oncology. 16 (4): 426–435. doi:10.1016/S1470-2045(15)70081-1. hdl:2318/1534804. PMID 25795408.

External links

Media related to Linsitinib at Wikimedia Commons

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[1] Mulvihill MJ, Cooke A, Rosenfeld-Franklin M, Buck E, Foreman K, Landfair D, et al. (September 2009). "Discovery of OSI-906: a selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor". Future Medicinal Chemistry. 1 (6): 1153–1171. doi:10.4155/fmc.09.89. PMID 21425998.

[2] "Linsitinib". Cancer.gov. National Cancer Institute. Retrieved October 16, 2012.

[springer.com-3] 1 2 3 "Linsitinib - Sling Therapeutics". AdisInsight. Springer Nature Switzerland AG.

[4] Fassnacht M, Berruti A, Baudin E, Demeure MJ, Gilbert J, Haak H, et al. (April 2015). "Linsitinib (OSI-906) versus placebo for patients with locally advanced or metastatic adrenocortical carcinoma: a double-blind, randomised, phase 3 study". The Lancet Oncology. 16 (4): 426–435. doi:10.1016/S1470-2045(15)70081-1. hdl:2318/1534804. PMID 25795408.

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