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Drug

Sapanisertib

Early clinical development
ClassSerine/threonine-protein kinase mTOR inhibitor
RxNorm2395271ChEMBLCHEMBL3545097UNIIJGH0DF1U03
10
Active clinical trials
MTOR
Primary target
Latest activity
beta

Recent clinical, regulatory, research and industry developments relating to this drug.

A Phase I/II Trial of Sapanisertib in Combination With Cabozantinib in ß-catenin-mutated Hepatocellular Carcinoma (SAPHIRE)

Clinical trial2026-08-26Results expected Q3 2027 · ClinicalTrials.gov

Molecular Analysis for Therapy Choice (MATCH)

Clinical trial2026-08-04Results expected Q4 2026 · ClinicalTrials.gov

Open-Label Umbrella Study to Evaluate Safety and Efficacy of Sapanisertib and Serabelisib (PIKTOR) in Various Combinations in Patients With HR+/HER2- Advanced or Metastatic Breast Cancer

Clinical trial2026-07-02Results expected Q2 2029 · ClinicalTrials.gov

A Phase 1 Study of MLN0128 and Bevacizumab in Patients With Recurrent Glioblastoma and Other Solid Tumors

Clinical trial2026-06-26Results posted · ClinicalTrials.gov

A Phase 1 Trial of MLN0128 (TAK-228) in Combination With Osimertinib (AZD9291) in Advanced EGFR Mutation Positive Non-Small Cell Lung Cancer (NSCLC) After Progression on a Previous EGFR Tyrosine Kinase Inhibitor

Clinical trial2026-06-11Results expected Q1 2027 · ClinicalTrials.gov

A Phase 1 Trial of MLN0128 (Sapanisertib) and CB-839 HCl (Telaglenastat) in Advanced NSCLC Patients

Clinical trial2026-05-26Results posted · ClinicalTrials.gov

An Open Label, Multicenter, Single Arm Phase II Study to Evaluate the Activity and Tolerability of the Novel mTOR Inhibitor, MLN0128 (TAK-228), in Patients With Locally Advanced or Metastatic Transitional Cell Carcinoma of the Urothelial Tract Whose Tumors Harbor a TSC1 and/or a TSC2 Mutation

Clinical trial2026-05-13Results posted · ClinicalTrials.gov

MATCH Treatment Subprotocol L: Phase II Study of MLN0128 (TAK-228) in Patients With Tumors Wtih mTOR Mutations

Clinical trial2026-05-13Results expected Q4 2026 · ClinicalTrials.gov

MATCH Treatment Subprotocol M: Phase II Study of MLN0128 (Tak-228) in Patients With Tumors With TSC1 or TSC2 Mutations

Clinical trial2026-05-13Results expected Q4 2026 · ClinicalTrials.gov

An Open-label, Multi-Center, Phase 2 Clinical Trial Evaluating Sapanisertib and Serabelisib (PIKTOR) With Paclitaxel, and a Substudy Evaluating PIKTOR With Paclitaxel Plus an Insulin-Suppressing Diet, in Patients With Advanced or Recurrent Endometrial Cancer

Clinical trial2025-12-24Results expected Q3 2028 · ClinicalTrials.gov

Phase I Study of MLN0128 (TAK-228) (NSC# 768435) in Combination With Ziv-Aflibercept (NSC# 724770) in Patients With Advanced Cancers

Clinical trial2025-10-20Results posted · ClinicalTrials.gov

A Phase 2 Study of MLN0128 (TAK-228) in Relapsed and/or Refractory Acute Lymphoblastic Leukemia (ALL)

Clinical trial2025-03-03Results posted · ClinicalTrials.gov

Profile

Identifiers & mechanism

Canonical identifiers, marketed brand names and mechanism, resolved across RxNorm, ChEMBL and ATC.

Canonical name
Sapanisertib
RxNorm CUI
2395271
ChEMBL ID
CHEMBL3545097
UNII
JGH0DF1U03
Primary mechanism
Serine/threonine-protein kinase mTOR inhibitor

Pharmacology & targets

1 target

Known molecular targets and mechanisms supported by curated pharmacology databases.

Serine/threonine-protein kinase mTOR
MTOR · P42345
INHIBITORSerine/threonine-protein kinase mTOR inhibitor

Clinical trials

27 trials

The current development programme across all trial phases — status mix, phase distribution and the late-stage studies shaping the evidence base.

Development programme
CLINICALTRIALS.GOV · LIVE REGISTRY
27
registered trials across all phases
LATEST COMPLETION 2024
10
Active studies
3
Recruiting
12
Completed
5
Discontinued
PHASE DISTRIBUTIONn = 27
Phase 110Phase 1 / 24Phase 213

Recent completions

Trials that read out recently, adding to the completed evidence base.

A Phase 2 Study of MLN0128 (TAK-228) in Relapsed and/or Refractory Acute Lymphoblastic Leukemia (ALL)

CompletedPH IINational Cancer Institute (NCI)n=162024

Phase I Study of MLN0128 (TAK-228) (NSC# 768435) in Combination With Ziv-Aflibercept (NSC# 724770) in Patients With Advanced Cancers

CompletedPH INational Cancer Institute (NCI)n=832024

A Ph1b Study of Osimertinib + Alisertib or Sapanisertib for Osimertinib-Resistant EGFR Mutant Non-Small Cell Lung Cancer (NSCLC) (Crossover Study)

CompletedPH IM.D. Anderson Cancer Centern=372023

A Phase II Study of MLN0128 (TAK-228) in Rapalog-Resistant Advanced Pancreatic Neuroendocrine Tumors (PNET)

CompletedPH IINational Cancer Institute (NCI)n=132022

Phase I Study of TAK-228 (MLN0128) in Combination With Metformin in Patients With Advanced Cancers

CompletedPH IM.D. Anderson Cancer Centern=312022

A Phase I Study of TAK-228 (MLN0128) in Combination With Carboplatin Plus Paclitaxel in Patients With Advanced Malignancies

CompletedPH IM.D. Anderson Cancer Centern=352022
References & data sources
  • RxNorm (U.S. National Library of Medicine) — drug identity
  • ChEMBL (EMBL-EBI) & UniProt — pharmacology and targets
  • ClinicalTrials.gov — clinical trials