Linsitinib
Names | |
---|---|
Preferred IUPAC name (1s,3s)-3-[8-Amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl]-1-methylcyclobutan-1-ol | |
Other names OSI-906 | |
Identifiers | |
CAS Number |
|
3D model (JSmol) |
|
ChEBI |
|
ChEMBL |
|
ChemSpider |
|
DrugBank |
|
KEGG |
|
PubChem CID |
|
UNII |
|
CompTox Dashboard (EPA) |
|
InChI
| |
| |
Properties | |
Chemical formula | C26H23N5O |
Molar mass | 421.504 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). Infobox references |
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, Mark J; Cooke, Andrew; Rosenfeld-Franklin, Maryland; Buck, Elizabeth; Foreman, Ken; Landfair, Darla; O’Connor, Matthew; Pirritt, Caroline; Sun, Yingchaun; Yao, Yan; Arnold, Lee D; Gibson, Neil W; Ji, Qun-Sheng (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". NCI Drug Dictionary. National Cancer Institute. Retrieved October 16, 2012.
- ^ a b c "Linsitinib - AdisInsight". adisinsight.springer.com.
- ^ Fassnacht, Martin; Berruti, Alfredo; Baudin, Eric; Demeure, Michael J; Gilbert, Jill; Haak, Harm; Kroiss, Matthias; Quinn, David I; Hesseltine, Elizabeth; Ronchi, Cristina L; Terzolo, Massimo; Toni Choueiri; Poondru, Srinivasu; Fleege, Tanya; Rorig, Ramona; Chen, Jihong; Stephens, Andrew W; Worden, Francis; Hammer, Gary D (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
- v
- t
- e
- Agonists: Angiopoietin 1
- Angiopoietin 4
- Antagonists: Angiopoietin 2
- Angiopoietin 3
- Kinase inhibitors: Altiratinib
- CE-245677
- Rebastinib
- Antibodies: Evinacumab (against angiopoietin 3)
- Nesvacumab (against angiopoietin 2)
EGF (ErbB1/HER1) |
|
---|---|
ErbB2/HER2 |
|
ErbB3/HER3 |
|
ErbB4/HER4 |
|
FGFR1 | |
---|---|
FGFR2 |
|
FGFR3 | |
FGFR4 | |
Unsorted |
|
- Agonists: Fosgonimeton
- Hepatocyte growth factor
- Potentiators: Dihexa (PNB-0408)
- Kinase inhibitors: Altiratinib
- AM7
- AMG-458
- Amuvatinib
- BMS-777607
- Cabozantinib
- Capmatinib
- Crizotinib
- Foretinib
- Golvatinib
- INCB28060
- JNJ-38877605
- K252a
- MK-2461
- PF-04217903
- PF-2341066
- PHA-665752
- SU-11274
- Tivantinib
- Volitinib
- Antibodies: Emibetuzumab
- Ficlatuzumab
- Flanvotumab
- Onartuzumab
- Rilotumumab
- Telisotuzumab
- Telisotuzumab vedotin
IGF-1 |
|
---|---|
IGF-2 |
|
Others |
- Antagonists: ALE-0540
- Dexamethasone
- EVT-901 (SAR-127963)
- Testosterone
- Antibodies: Against NGF: ABT-110 (PG110)
- ASP-6294
- Fasinumab
- Frunevetmab
- Fulranumab
- MEDI-578
- Ranevetmab
- Tanezumab
- Aptamers: Against NGF: RBM-004
- Decoy receptors: LEVI-04 (p75NTR-Fc)
- Agonists: Becaplermin
- Platelet-derived growth factor (A, B, C, D)
- Kinase inhibitors: Agerafenib
- Avapritinib
- Axitinib
- Crenolanib
- Imatinib
- Lenvatinib
- Masitinib
- Motesanib
- Nintedanib
- Pazopanib
- Radotinib
- Quizartinib
- Ripretinib
- Sunitinib
- Sorafenib
- Toceranib
- Antibodies: Olaratumab
- Ramucirumab
- Tovetumab
GFRα1 |
|
---|---|
GFRα2 |
|
GFRα3 |
|
GFRα4 |
|
Unsorted |
|
- See here instead.
TrkA |
|
---|---|
TrkB |
|
TrkC |
|
- Agonists: Placental growth factor (PGF)
- Ripretinib
- Telbermin
- VEGF (A, B, C, D (FIGF))
- Allosteric modulators: Cyclotraxin B
- Kinase inhibitors: Agerafenib
- Altiratinib
- Axitinib
- Cabozantinib
- Cediranib
- Fruquintinib
- Lapatinib
- Lenvatinib
- Motesanib
- Nintedanib
- Pazopanib
- Pegaptanib
- Rebastinib
- Regorafenib
- Semaxanib
- Sorafenib
- Sunitinib
- Toceranib
- Tivozanib
- Vandetanib
- WHI-P 154
- Antibodies: Alacizumab pegol
- Bevacizumab
- Icrucumab
- Ramucirumab
- Ranibizumab
- Decoy receptors: Aflibercept
- Additional growth factors: Adrenomedullin
- Colony-stimulating factors (see here instead)
- Connective tissue growth factor (CTGF)
- Ephrins (A1, A2, A3, A4, A5, B1, B2, B3)
- Erythropoietin (see here instead)
- Glucose-6-phosphate isomerase (GPI; PGI, PHI, AMF)
- Glia maturation factor (GMF)
- Hepatoma-derived growth factor (HDGF)
- Interleukins/T-cell growth factors (see here instead)
- Leukemia inhibitory factor (LIF)
- Macrophage-stimulating protein (MSP; HLP, HGFLP)
- Midkine (NEGF2)
- Migration-stimulating factor (MSF; PRG4)
- Oncomodulin
- Pituitary adenylate cyclase-activating peptide (PACAP)
- Pleiotrophin
- Renalase
- Thrombopoietin (see here instead)
- Wnt signaling proteins
- Additional growth factor receptor modulators: Cerebrolysin (neurotrophin mixture)
This antineoplastic or immunomodulatory drug article is a stub. You can help Wikipedia by expanding it. |
- v
- t
- e