[[File:Linsitinib.svg|thumb|right|Chemical structure of Linsitinib]]
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'''Linsitinib''' is an experimental drug candidate for the treatment of various types of cancer. It is an [[enzyme inhibitor|inhibitor]] of the [[insulin receptor]] and of the [[insulin-like growth factor 1 receptor]] (IGF-1R).<ref>{{cite journal | pmid = 21425998 | year = 2009 | last1 = Mulvihill | first1 = MJ | last2 = Cooke | first2 = A | last3 = Rosenfeld-Franklin | first3 = M | last4 = Buck | first4 = E | last5 = Foreman | first5 = K | last6 = Landfair | first6 = D | last7 = O'Connor | first7 = M | last8 = Pirritt | first8 = C | last9 = Sun | first9 = Y | last10 = Yao | first10 = Yan | last11 = Arnold | first11 = Lee D | last12 = Gibson | first12 = Neil W | last13 = Ji | first13 = Qun-Sheng | title = Discovery of OSI-906: A selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor | volume = 1 | issue = 6 | pages = 1153–71 | doi = 10.4155/fmc.09.89 | journal = [[Future Medicinal Chemistry]]| display-authors = 8 }}</ref> This prevents tumor cell proliferation and induces tumor cell [[apoptosis]].<ref>{{cite web | url = http://www.cancer.gov/drugdictionary?cdrid=566191 | title = Linsitinib | work = NCI Drug Dictionary | publisher = [[National Cancer Institute]] | accessdate = October 16, 2012}}</ref>
'''Linsitinib''' is a small molecule inhibitor that targets the [[insulin-like growth factor 1 receptor]] (IGF-1R) and the [[insulin receptor]] (IR). It is primarily investigated for its potential use in the treatment of various types of [[cancer]].
Linsitinib was granted [[orphan drug designation]] for adrenocortical carcinoma in March 2012.<ref name="springer.com">{{cite web|url=http://adisinsight.springer.com/drugs/800026466|title=Linsitinib - AdisInsight|website=adisinsight.springer.com}}</ref>
== Mechanism of Action ==
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.<ref name="springer.com"/> A phase III clinical trial found that linsitinib did not increase survival in patients with adrenocortical carcinoma.<ref>{{cite journal|url=http://www.thelancet.com/journals/lanonc/article/PIIS1470-2045(15)70081-1/abstract|title=Linsitinib (OSI-906) versus placebo for patients with locally advanced or metastatic adrenocortical carcinoma: a double-blind, randomised, phase 3 study|vauthors=Fassnacht M, Berruti A, Baudin E, Demeure MJ, Gilbert J, Haak H, Kroiss M, Quinn DI, Hesseltine E, Ronchi CL, Terzolo M, Choueiri TK, Poondru S, Fleege T, Rorig R, Chen J, Stephens AW, Worden F, Hammer GD|date=1 April 2015|journal=The Lancet Oncology|volume=16|issue=4|pages=426–435|doi=10.1016/S1470-2045(15)70081-1|pmid=25795408|hdl=2318/1534804}}</ref> As of 2017, no clinical trials were in progress.<ref name="springer.com"/>
Linsitinib functions by inhibiting the activity of IGF-1R and IR, which are both [[tyrosine kinase]] receptors. These receptors play a crucial role in the regulation of cell growth, survival, and differentiation. By blocking these receptors, linsitinib can interfere with the signaling pathways that promote [[tumor]] growth and proliferation.
==References==
== Clinical Applications ==
{{Reflist}}
{{Growth factor receptor modulators}}
Linsitinib has been studied in clinical trials for its efficacy in treating several types of cancer, including [[adrenocortical carcinoma]], [[non-small cell lung cancer]], and [[breast cancer]]. The drug's ability to inhibit IGF-1R and IR makes it a promising candidate for targeting tumors that rely on these pathways for growth.
[[Category:Experimental cancer drugs]]
== Side Effects ==
[[Category:Quinolines]]
[[Category:Protein kinase inhibitors]]
[[Category:Astellas Pharma]]
[[Category:Cyclobutanes]]
[[Category:Imidazopyrazines]]
As with many cancer therapies, linsitinib can cause a range of side effects. Common side effects include [[nausea]], [[fatigue]], and [[diarrhea]]. More serious side effects may include [[hyperglycemia]] due to its action on the insulin receptor.
{{antineoplastic-drug-stub}}
== Research and Development ==
Research on linsitinib is ongoing, with studies focusing on its effectiveness as a monotherapy and in combination with other anticancer agents. The drug's development highlights the importance of targeting specific molecular pathways in cancer treatment.
Linsitinib functions by inhibiting the activity of IGF-1R and IR, which are both tyrosine kinase receptors. These receptors play a crucial role in the regulation of cell growth, survival, and differentiation. By blocking these receptors, linsitinib can interfere with the signaling pathways that promote tumor growth and proliferation.
Linsitinib has been studied in clinical trials for its efficacy in treating several types of cancer, including adrenocortical carcinoma, non-small cell lung cancer, and breast cancer. The drug's ability to inhibit IGF-1R and IR makes it a promising candidate for targeting tumors that rely on these pathways for growth.
As with many cancer therapies, linsitinib can cause a range of side effects. Common side effects include nausea, fatigue, and diarrhea. More serious side effects may include hyperglycemia due to its action on the insulin receptor.
Research on linsitinib is ongoing, with studies focusing on its effectiveness as a monotherapy and in combination with other anticancer agents. The drug's development highlights the importance of targeting specific molecular pathways in cancer treatment.
