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Drugs / Sapanisertib
last change Aug 2026 re-read 9 days ago

Sapanisertib

also known as TAK-228 · MLN0128 · CB-228 · INK128

Small molecule targets MTOR via inhibition

Developed for
non-small cell lung carcinoma · plasma cell myeloma · endometrial cancer · fallopian tube carcinoma · female breast carcinoma · hepatocellular carcinoma · metastatic malignant neoplasm · neoplasm
+61 more · non-small cell squamous lung carcinoma · ovarian carcinoma · ovarian endometrioid adenocarcinoma · prostate carcinoma · urinary bladder carcinoma · urothelial carcinoma · adult acute lymphoblastic leukemia · adult glioblastoma · adult lymphoma · anaplastic large cell lymphoma · B-cell acute lymphoblastic leukemia · B-lymphoblastic leukemia/lymphoma with t(9;22)(q34.1;q11.2) · breast cancer · breast neoplasm · cancer · cancer-related condition · classic Hodgkin lymphoma · clear cell renal carcinoma · cutaneous neuroendocrine carcinoma · differentiated thyroid carcinoma · digestive system cancer · endometrial clear cell adenocarcinoma · endometrial serous adenocarcinoma · estrogen-receptor positive breast cancer · female reproductive organ cancer · fibrolamellar hepatocellular carcinoma · head and neck cancer · high grade malignant neoplasm · hormone receptor-positive breast cancer · leiomyosarcoma of the corpus uteri · lymphoma · male reproductive organ cancer · malignant peripheral nerve sheath tumor · metastatic malignant neoplasm in the brain · myxofibrosarcoma · neoplastic disease or syndrome · neoplastic meningitis · ovarian carcinosarcoma · ovarian clear cell adenocarcinoma · ovarian clear cell cystadenocarcinoma · ovarian mucinous cystadenocarcinoma · ovarian serous adenocarcinoma · ovarian serous cystadenocarcinoma · pancreatic endocrine carcinoma · pancreatic neuroendocrine tumor · pancreatic neuroendocrine tumor G1 · peripheral T-cell lymphoma, not otherwise specified · primary peritoneal carcinoma · primary peritoneal serous adenocarcinoma · refractory malignant neoplasm · renal cell carcinoma · secondary malignant neoplasm · soft tissue sarcoma · squamous cell lung carcinoma · synovial sarcoma · T-cell acute lymphoblastic leukemia · thyroid gland undifferentiated (anaplastic) carcinoma · triple-negative breast carcinoma · undifferentiated pleomorphic sarcoma · Waldenstrom macroglobulinemia · glioblastoma
Investigated by
National Cancer Institute (NCI) · Millennium Pharmaceuticals, Inc. · M.D. Anderson Cancer Center · Calithera Biosciences, Inc · Takeda · Faeth Therapeutics
+20 more · Dana-Farber Cancer Institute · Associació per a la Recerca Oncologica, Spain · Avera McKennan Hospital & University Health Center · Big Ten Cancer Research Consortium · Bradley A. McGregor, MD · European Network of Individualized Treatment in Endometrial Cancer - ENITEC · European Network of Translational Research in Ovarian Cancer - EUTROC · Fox Chase Cancer Center · GOG Foundation · Gary Schwartz · Imperial College London · Joyce O'Shaughnessy · Kathy Miller · Memorial Sloan Kettering Cancer Center · North Eastern German Society of Gynaecological Oncology · Pivotal S.L. · SWOG Cancer Research Network · Takeda Pharmaceuticals International, Inc. · The Methodist Hospital Research Institute · University of Colorado, Denver

Trials 50

today NCT07558733 · Ph 1/2 NCT06811116 · Ph 1/2 NCT06463028 · Ph 2 NCT05275673 · Ph 2 NCT05022394 · Ph 1/2 NCT04250545 · Ph 1 NCT04267913 · Ph 2 NCT04479306 · Ph 1 NCT03648489 · Ph 2 NCT03745911 · Ph 2 NCT03205891 · Ph 1 NCT03430882 · Ph 1 NCT03017833 · Ph 1 NCT03370302 · Ph 1 NCT03047213 · Ph 2 NCT03097328 · Ph 2 NCT03193853 · Ph 2 NCT03154294 · Ph 1 NCT02893930 · Ph 2 NCT02988986 · Ph 2 NCT02619669 · Ph 1 NCT02484430 · Ph 2 NCT02503722 · Ph 1 NCT06385496 · Ph 2 NCT06390865 · Ph 2 NCT02727777 · Ph 1/2 NCT02987959 · Ph 2 NCT02417701 · Ph 2 NCT02812056 · Ph 1 NCT02756364 · Ph 2 NCT02575339 · Ph 1/2 NCT02724020 · Ph 2 NCT02719691 · Ph 1 NCT02725268 · Ph 2 NCT02601209 · Ph 1/2 NCT02514824 · Ph 1/2 NCT02465060 · Ph 2 NCT02244463 · Ph 1/2 NCT02412722 · Ph 1 NCT02327169 · Ph 1 NCT02197572 · Ph 1 NCT02133183 · Ph 1 NCT02159989 · Ph 1 NCT02142803 · Ph 1 NCT02091531 · Ph 2 NCT02049957 · Ph 2 NCT01899053 · Ph 1 NCT01351350 · Ph 1 NCT01118689 · Ph 1 NCT01058707 · Ph 1
20102011201220132014201520162017201820192020202120222023202420252026202720282029
PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 121 trials
Phase 1 NCT04250545 Oct 2020 → Nov 2025 overdue metastatic malignant neoplasm in the brain, neoplastic meningitis, non-small cell lung carcinoma National Cancer Institute (NCI) Active not recruiting No outcome recorded
Phase 1 NCT04479306 Jun 2020 → Jul 2023 non-small cell lung carcinoma M.D. Anderson Cancer Center Completed No outcome recorded
Phase 1 NCT03430882 Mar 2018 → Jun 2022 refractory malignant neoplasm, secondary malignant neoplasm M.D. Anderson Cancer Center Completed No outcome recorded
Phase 1 NCT03017833 Mar 2018 → Dec 2022 metastatic malignant neoplasm M.D. Anderson Cancer Center Completed No outcome recorded
Phase 1 NCT03205891 Mar 2018 → Mar 2021 anaplastic large cell lymphoma, classic Hodgkin lymphoma, peripheral T-cell lymphoma, not otherwise specified M.D. Anderson Cancer Center Withdrawn No outcome recorded
Phase 1 NCT03370302 Jan 2018 → Aug 2019 neoplasm Calithera Biosciences, Inc Terminated No outcome recorded Stop: Enrollment
Phase 1 NCT03154294 Jul 2017 → Nov 2020 — Avera McKennan Hospital & University Health Center Completed No outcome recorded
Phase 1 NCT02619669 Apr 2017 → Jun 2019 female breast carcinoma Gary Schwartz Withdrawn No outcome recorded Stop: Enrollment
Phase 1 NCT02503722 Mar 2017 → Feb 2027 expected non-small cell lung carcinoma National Cancer Institute (NCI) Active not recruiting No outcome recorded
Phase 1 NCT02812056 Sep 2016 → Sep 2021 digestive system cancer, female reproductive organ cancer, head and neck cancer, male reproductive organ cancer M.D. Anderson Cancer Center Withdrawn No outcome recorded
Phase 1/28 trials · 1 missed
Phase 1/2 NCT07558733 Apr 2026 → May 2029 expected hormone receptor-positive breast cancer Faeth Therapeutics Recruiting No outcome recorded
Phase 1/2 NCT06811116 Nov 2025 → Aug 2027 expected hepatocellular carcinoma National Cancer Institute (NCI) Recruiting No outcome recorded
Phase 1/2 NCT05022394 Feb 2021 non-small cell lung carcinoma M.D. Anderson Cancer Center Withdrawn No outcome recorded Stop: Enrollment
Phase 1/2 NCT02727777 Mar 2017 → Jul 2018 lymphoma M.D. Anderson Cancer Center Terminated No outcome recorded Stop: Enrollment
Phase 1/2 NCT02575339 Jul 2016 → Jun 2018 hepatocellular carcinoma Kathy Miller Terminated No outcome recorded Stop: Business
Phase 1/2 NCT02601209 Nov 2015 → Dec 2018 leiomyosarcoma of the corpus uteri, malignant peripheral nerve sheath tumor, myxofibrosarcoma, synovial sarcoma +1 National Cancer Institute (NCI) Terminated Missed primary
Phase 1/2 NCT02514824 Oct 2015 → Apr 2017 cutaneous neuroendocrine carcinoma Dana-Farber Cancer Institute Completed No outcome recorded
Phase 1/2 NCT02244463 Jul 2015 → Apr 2022 differentiated thyroid carcinoma, thyroid gland undifferentiated (anaplastic) carcinoma Dana-Farber Cancer Institute Completed No outcome recorded
Phase 221 trials · 3 missed
Phase 2 NCT06463028 Dec 2024 → Sep 2028 expected endometrial cancer Faeth Therapeutics Recruiting No outcome recorded
Phase 2 NCT05275673 Jul 2022 → Jan 2023 non-small cell squamous lung carcinoma Faeth Therapeutics Terminated No outcome recorded Stop: Business
Phase 2 NCT04267913 Sep 2020 → Oct 2025 squamous cell lung carcinoma SWOG Cancer Research Network Withdrawn No outcome recorded
Phase 2 NCT03648489 Sep 2018 → Nov 2023 fallopian tube carcinoma, ovarian carcinosarcoma, ovarian clear cell adenocarcinoma, ovarian endometrioid adenocarcinoma +2 Imperial College London Completed No outcome recorded
Phase 2 NCT03745911 May 2018 → Nov 2020 urothelial carcinoma Associació per a la Recerca Oncologica, Spain Unknown No outcome recorded
Phase 2 NCT03047213 Aug 2017 → Oct 2020 overdue urinary bladder carcinoma, urothelial carcinoma National Cancer Institute (NCI) Active not recruiting No outcome recorded
Phase 2 NCT03097328 Aug 2017 → Jul 2021 renal cell carcinoma Bradley A. McGregor, MD Completed No outcome recorded
Phase 2 NCT03193853 Jul 2017 → Mar 2020 triple-negative breast carcinoma Joyce O'Shaughnessy Completed No outcome recorded
Phase 2 NCT02893930 Apr 2017 → May 2021 pancreatic endocrine carcinoma, pancreatic neuroendocrine tumor G1 National Cancer Institute (NCI) Completed No outcome recorded
Phase 2 NCT02988986 Apr 2017 → Feb 2019 estrogen-receptor positive breast cancer The Methodist Hospital Research Institute Completed No outcome recorded

News releases announcing trial results or a regulatory action · 1

DateIssuerRelease
2026-08-17 Faeth Therapeutics Regulatory Faeth Therapeutics Announces FDA Grant of Fast Track Designation for PIKTOR Plus Paclitaxel in Biomarker-Selected Advanced Endometrial Cancer faeththerapeutics.com ↗
Fast Track designation applies to sapanisertib and serabelisib (PIKTOR) in combination with paclitaxel for the treatment of patients with advanced or recurrent endometrial cancer whose tumors harbor a PI3K/AKT/mTOR pathway alteration

All press releases naming this drug 1 release

DateIssuerRelease

Evidence & citations 9 cited values

Every value below carries the sentence it was read from. 53 sources stand behind the page.

FieldValueCited text
Known as Sapanisertib “Patients with previously treated advanced solid tumors were eligible for this open label, cohort study of sapanisertib (TAK-228) and serabelisib (TAK-117) with weekly paclitaxel.” PMID 35843739 ↗ Jul 2022
30

“Phase 1 study of mTORC1/2 inhibitor sapanisertib (TAK-228) in advanced solid tumours, with an expansion phase in renal, endometrial or bladder cancer.” PMID 32913286 ↗ Sep 2020

“A Phase 1 Study of Sapanisertib (TAK-228) in East Asian Patients with Advanced Nonhematological Malignancies.” PMID 34843044 ↗ Nov 2021

“Biomarker-Based Phase II Study of Sapanisertib (TAK-228): An mTORC1/2 Inhibitor” PMID 35171658 ↗ Feb 2022

NCT02142803 ↗

NCT02601209 ↗

NCT02133183 ↗

NCT05022394 ↗

NCT02412722 ↗

NCT07558733 ↗

NCT02756364 ↗

Show 20 more sources
Known as CB-228 “Sapanisertib (CB-228/TAK-228) is a potent, selective ATP-competitive, dual inhibitor of mTORC1/2.” PMID 38126764 ↗ Feb 2024
Known as INK128 “TAK-228 (formerly INK128 or MLN0128) targets 2 distinct multiprotein complexes, mTORC1 and mTORC2.” NCT02619669 ↗
Known as MLN0128 “TAK-228 (formerly INK128 or MLN0128) targets 2 distinct multiprotein complexes, mTORC1 and mTORC2.” NCT02619669 ↗
9

NCT01118689 ↗

NCT02719691 ↗

NCT02244463 ↗

NCT02514824 ↗

NCT02724020 ↗

NCT01351350 ↗

NCT02575339 ↗

NCT02091531 ↗

NCT02327169 ↗
Known as TAK-228 “Patients with previously treated advanced solid tumors were eligible for this open label, cohort study of sapanisertib (TAK-228) and serabelisib (TAK-117) with weekly paclitaxel.” PMID 35843739 ↗ Jul 2022
16

“TAK-228 (formerly MLN0128), an investigational dual TORC1/2 inhibitor plus paclitaxel, with/without trastuzumab, in patients with advanced solid malignancies.” PMID 28601972 ↗ Jun 2017

“Sapanisertib (TAK-228) is an investigational, orally available, potent and highly selective mTORC1/2 inhibitor demonstrating promise in numerous malignancies.” PMID 29464110 ↗ Feb 2018

“Phase 1 study of mTORC1/2 inhibitor sapanisertib (TAK-228) in advanced solid tumours, with an expansion phase in renal, endometrial or bladder cancer.” PMID 32913286 ↗ Sep 2020

“A Phase 1 Study of Sapanisertib (TAK-228) in East Asian Patients with Advanced Nonhematological Malignancies.” PMID 34843044 ↗ Nov 2021

“Biomarker-Based Phase II Study of Sapanisertib (TAK-228): An mTORC1/2 Inhibitor” PMID 35171658 ↗ Feb 2022

“Drug: Tak-228 & Tak-117” NCT03193853 ↗

NCT03193853 ↗

NCT02812056 ↗

NCT02619669 ↗

NCT03205891 ↗

Show 6 more sources
Action Inhibit “sapanisertib, an oral, highly selective inhibitor of mTORC1/mTORC2” PMID 32913286 ↗ Sep 2020
Modality Small molecule “Sapanisertib is a small molecule inhibitor of the mammalian mTOR serine/threonine kinase.” NCT07558733 ↗
Route Oral “MLN0128 administered orally once daily for 28 days” NCT01118689 ↗
Target MTOR “sapanisertib, an oral, highly selective inhibitor of mTORC1/mTORC2” PMID 32913286 ↗ Sep 2020