Sapanisertib

{{Short description|Chemical compound}}

{{Infobox drug

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| IUPAC_name = 5-(4-Amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1,3-benzoxazol-2-amine

| image = Sapanisertib.svg

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| CAS_number = 1224844-38-5

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| UNII = JGH0DF1U03

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| PubChem = 45375953

| ChEBI = 91450

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| KEGG = D11183

| C=15|H=15|N=7|O=1

| StdInChI=1S/C15H15N7O/c1-7(2)22-14-11(13(16)18-6-19-14)12(21-22)8-3-4-10-9(5-8)20-15(17)23-10/h3-7H,1-2H3,(H2,17,20)(H2,16,18,19)

| StdInChIKey=GYLDXIAOMVERTK-UHFFFAOYSA-N

| smiles = CC(C)N1C2=C(C(=N1)C3=CC4=C(C=C3)OC(=N4)N)C(=NC=N2)N

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Sapanisertib (also known as MLN0128, INK128 and TAK-228) is an experimental small molecule inhibitor of mTOR which is administered orally. It targets both mTORC1 and mTORC2.{{cite journal | vauthors = Panchal II, Badeliya SN, Patel R, Patel A, Devaligar A | title = In silico Analysis and Molecular Docking Studies of Novel 4-Amino-3- (Isoquinolin-4-yl)-1H-Pyrazolo[3,4-d]Pyrimidine Derivatives as Dual PI3-K/mTOR Inhibitors | journal = Current Drug Discovery Technologies | year = 2019 | volume = 16 | issue = 3 | pages = 297–306 | pmid = 30387396 | doi = 10.2174/1568009618666181102144934 | s2cid = 54344624 }}

Developed by Millennium Pharmaceuticals,{{cite journal | vauthors = Guo N, Azadniv M, Coppage M, Nemer M, Mendler J, Becker M, Liesveld J | title = Effects of Neddylation and mTOR Inhibition in Acute Myelogenous Leukemia | journal = Translational Oncology | volume = 12 | issue = 4 | pages = 602–613 | date = April 2019 | pmid = 30699367 | doi = 10.1016/j.tranon.2019.01.001 | pmc = 6348338 }}{{cite journal | vauthors = Ouvry G, Clary L, Tomas L, Aurelly M, Bonnary L, Borde E, Bouix-Peter C, Chantalat L, Defoin-Platel C, Deret S, Forissier M, Harris CS, Isabet T, Lamy L, Luzy AP, Pascau J, Soulet C, Taddei A, Taquet N, Thoreau E, Varvier E, Vial E, Hennequin LF | display-authors = 6 | title = Impact of Minor Structural Modifications on Properties of a Series of mTOR Inhibitors | journal = ACS Medicinal Chemistry Letters | volume = 10 | issue = 11 | pages = 1561–1567 | date = November 2019 | pmid = 31749911 | doi = 10.1021/acsmedchemlett.9b00401 | pmc = 6862343 }}{{cite journal | vauthors = Arnold A, Yuan M, Price A, Harris L, Eberhart CG, Raabe EH | title = Synergistic activity of mTORC1/2 kinase and MEK inhibitors suppresses pediatric low-grade glioma tumorigenicity and vascularity | journal = Neuro-Oncology | volume = 22 | issue = 4 | pages = 563–574 | date = April 2020 | pmid = 31841591 | doi = 10.1093/neuonc/noz230 | pmc = 7158655 }} and is in phase II clinical trials for breast cancer, endometrial cancer, glioblastoma, renal cell carcinoma, and thyroid cancer.{{cite web | title = Sapanisertib - Takeda Oncology | url = http://adisinsight.springer.com/drugs/800030541 | work = Adis Insight | publisher = Springer Nature Switzerland AG }} The drug has been well tolerated by patients with advanced solid tumours in Phase I trials.{{cite journal | vauthors = Moore KN, Bauer TM, Falchook GS, Chowdhury S, Patel C, Neuwirth R, Enke A, Zohren F, Patel MR | display-authors = 6 | title = Phase I study of the investigational oral mTORC1/2 inhibitor sapanisertib (TAK-228): tolerability and food effects of a milled formulation in patients with advanced solid tumours | journal = ESMO Open | volume = 3 | issue = 2 | pages = e000291 | date = February 2018 | pmid = 29464110 | doi = 10.1136/esmoopen-2017-000291 | pmc = 5812400 | doi-access = free }}