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Sapanisertib

Phase 2Small molecule

CCalithera Biosciences, Inc

Sapanisertib is an experimental cancer drug being tested to treat various types of cancer by blocking proteins that help cancer cells grow and survive.[1] Sapanisertib is currently being investigated across 8 indications[3], with its most advanced program in Phase 2.[1]

Sapanisertib is one of 206 small molecule programs targeting Adult Glioblastoma. It is currently in Phase 2.

8

Indications

27

Total Trials

10

Active Trials

205

Competitors

Pipeline

Status by Indication[3][1]

Indication

Adult GlioblastomaActive, not recruiting

Breast CarcinomaRecruiting

Non-Small Cell Lung CancerWithdrawn

Endometrial CancerCompleted

TreatmentActive, not recruiting

Advanced Hepatocellular CarcinomaRecruiting

Advanced LymphomaActive, not recruiting

Locally Advanced Bladder Urothelial CarcinomaActive, not recruiting

Adult GlioblastomaPhase 1

Active, not recruiting

Breast CarcinomaPreclinical

Recruiting

Non-Small Cell Lung CancerPhase 2

Withdrawn

Endometrial CancerPhase 2

Completed

TreatmentPhase 2

Active, not recruiting

Advanced Hepatocellular CarcinomaPreclinical

Recruiting

Advanced LymphomaPhase 2

Active, not recruiting

Locally Advanced Bladder Urothelial CarcinomaPhase 2

Active, not recruiting

Competition

Competitive Landscape

414 competitors in Non-Small Cell Lung Cancer

#DrugCompanyPhaseTrials

Opdualag

Bristol-Myers Squibb

Oleclumab

Cadonilimab

SShanghai Pharmaceuticals Holding Co., Ltd

Sapanisertib

CCalithera Biosciences, Inc

Remeron

OOrganon and Co

Aqupla

Jiangsu Simcere Pharmaceutical Co., Ltd.

Ftorafur

TThe First Affiliated Hospital with Nanjing Medical University

Vibramycin

PPfizer's Upjohn has merged with Mylan to form Viatris Inc.

Treatment

PD-1 Inhibitors

BBioNTech US Inc.

Ranked by pipeline maturity and clinical activity. Current drug highlighted in teal.

Timeline

Expected Milestones

Q4 2026

Phase 2Active, not recruiting

Locally Advanced Bladder Urothelial Carcinoma

NCT03047213

Phase 1Active, not recruiting

Non-Small Cell Lung Cancer

NCT04250545

Phase 2Active, not recruiting

Treatment

NCT06390865

Phase 2Active, not recruiting

Advanced Lymphoma

NCT06385496

Q3 2027

PreclinicalRecruiting

Advanced Hepatocellular Carcinoma

NCT06811116

Q4 2027

Phase 2Active, not recruiting

Advanced Lymphoma

NCT02465060

Clinical

Trials by Indication[1]

Non-Small Cell Lung Cancer5 trials

Testing of the Anti Cancer Drugs CB-839 HCl (Telaglenastat) and MLN0128 (Sapanisertib) in Advanced Stage Non-small Cell Lung Cancer

Active, not recruiting·NNational Cancer Institute (NCI)·Phase 1·NCT04250545·22 enrolled

Testing the Combination of MLN0128 (TAK-228) and AZD9291 in Advanced EGFR (Epidermal Growth Factor Receptor) Mutation Positive Non-small Cell Lung Cancer

Active, not recruiting·NNational Cancer Institute (NCI)·Phase 1·NCT02503722·36 enrolled

A Study of Sapanisertib in Relapsed/Refractory NFE2L2-Mutated and Wild-Type Squamous Non-Small Cell Lung Cancer

Terminated·FFaeth Therapeutics·Phase 2·NCT05275673·7 enrolled

Show 2 more trials

Sapanisertib and Nivolumab for the Treatment of Stage I-IV Non-small Cell Lung Cancer in Patients Who Have Progressed on Prior PD-1/PD-L1 Inhibitor Therapy, I-OVERCOME Study

Withdrawn·MM.D. Anderson Cancer Center·Phase 1/2·NCT05022394

Osimertinib in Combination With Alisertib or Sapanisertib for the Treatment of Osimertinib-Resistant EGFR Mutant Stage IIIB or IV Non-Small Cell Lung Cancer

Completed·MM.D. Anderson Cancer Center·Phase 1·NCT04479306·37 enrolled

Endometrial Cancer2 trials

Sapanisertib and Serabelisib (PIKTOR) With Paclitaxel and a Substudy With an Insulin-Suppressing Diet in Patients With Advanced/Recurrent Endometrial Cancer

Recruiting·FFaeth Therapeutics·Phase 2·NCT06463028·40 enrolled

A Study of Sapanisertib, Combination of Sapanisertib With MLN1117, Paclitaxel and Combination of Sapanisertib With Paclitaxel in Women With Endometrial Cancer

Completed· Takeda logo

Takeda·Phase 2·NCT02725268·241 enrolled

Breast Cancer2 trials

Sapanisertib in Combination With Fulvestrant in Women With Advanced or Metastatic Breast Cancer After Aromatase Inhibitor Therapy

Completed·CCalithera Biosciences, Inc·Phase 2·NCT02756364·141 enrolled

Safety and Efficacy Study of Sapanisertib in Combination With Exemestane or Fulvestrant in Postmenopausal Women With Estrogen Receptor Positive/Human Epidermal Growth Factor Receptor 2 Negative (ER+/HER2-) Metastatic Breast Cancer

Completed·CCalithera Biosciences, Inc·Phase 2·NCT02049957·118 enrolled

Lung Cancer2 trials

Sapanisertib in Treating Patients With Stage IV or Recurrent Lung Cancer

Completed·NNational Cancer Institute (NCI)·Phase 2·NCT02417701·34 enrolled

Testing of TAK228 (MLN0128, Sapanisertib) Plus Docetaxel to the Usual Standard of Care for Advanced Squamous Cell Lung Cancer (A Lung-MAP Treatment Trial)

Withdrawn·SSWOG Cancer Research Network·Phase 2·NCT04267913

Advanced Lymphoma2 trials

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

Active, not recruiting·NNational Cancer Institute (NCI)·Phase 2·NCT06385496·35 enrolled

Molecular Analysis for Therapy Choice (MATCH)

Active, not recruiting·NNational Cancer Institute (NCI)·Phase 2·NCT02465060·6,452 enrolled

14 more indications

Relapsed or Refractory1 trial

Sapanisertib and Metformin in Treating Patients With Advanced or Metastatic Relapsed or Refractory Cancers

Completed·MM.D. Anderson Cancer Center·Phase 1·NCT03017833·31 enrolled

Pancreatic Neuroendocrine Tumor1 trial

Sapanisertib in Treating Patients With Metastatic or Refractory Pancreatic Neuroendocrine Tumor That Cannot Be Removed by Surgery

Completed·NNational Cancer Institute (NCI)·Phase 2·NCT02893930·13 enrolled

Advanced Solid Tumors1 trial

Effect of Sapanisertib (MLN0128) on the QTc Interval in Participants With Advanced Solid Tumors

Completed·CCalithera Biosciences, Inc·Phase 1·NCT02197572·44 enrolled

Metastatic Sarcoma1 trial

Sapanisertib or Pazopanib Hydrochloride in Treating Patients With Locally Advanced or Metastatic Sarcoma

Terminated·NNational Cancer Institute (NCI)·Phase 1/2·NCT02601209·151 enrolled

Hematologic Malignancies1 trial

A Safety, Tolerability, and Pharmacokinetics Study of MLN0128 as a Single Agent and in Combination With Paclitaxel in Adults With Advanced Nonhematologic Malignancies

Completed· Takeda logo

Takeda·Phase 1·NCT02412722·61 enrolled

Acute Lymphoblastic Leukemia1 trial

Sapanisertib in Treating Patients With Relapsed and/or Refractory Acute Lymphoblastic Leukemia

Completed·NNational Cancer Institute (NCI)·Phase 2·NCT02484430·16 enrolled

Treatment1 trial

Testing MLN0128 (TAK-228) as Potentially Targeted Treatment in Cancers With TSC1 or TSC2 Genetic Changes (MATCH - Subprotocol M)

Active, not recruiting·NNational Cancer Institute (NCI)·Phase 2·NCT06390865·49 enrolled

Solid Tumors1 trial

Sapanisertib and Ziv-Aflibercept in Treating Patients With Recurrent Solid Tumors That Are Metastatic or Cannot Be Removed by Surgery

Completed·NNational Cancer Institute (NCI)·Phase 1·NCT02159989·83 enrolled

Refractory Malignant Solid Tumors1 trial

Sapanisertib, Carboplatin, and Paclitaxel in Treating Patients With Recurrent or Refractory Malignant Solid Tumors

Completed·MM.D. Anderson Cancer Center·Phase 1·NCT03430882·35 enrolled

Glioblastoma1 trial

Sapanisertib Before and After Surgery in Treating Patients With Recurrent Glioblastoma

Terminated·NNational Cancer Institute (NCI)·Phase 1·NCT02133183·40 enrolled

Advanced Hepatocellular Carcinoma1 trial

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

Recruiting·NNational Cancer Institute (NCI)·Preclinical·NCT06811116·92 enrolled

Adult Glioblastoma1 trial

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

Active, not recruiting·NNational Cancer Institute (NCI)·Phase 1·NCT02142803·50 enrolled

Locally Advanced Bladder Urothelial Carcinoma1 trial

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

Active, not recruiting·NNational Cancer Institute (NCI)·Phase 2·NCT03047213·17 enrolled

Breast Carcinoma1 trial

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

Recruiting·FFaeth Therapeutics·Preclinical·NCT07558733·32 enrolled

Sources

References

[1]
ClinicalTrials.gov — 27 trial records for Sapanisertib. U.S. National Library of Medicine, National Institutes of Health.
[2]
ChEMBL — Sapanisertib compound record. European Bioinformatics Institute (EMBL-EBI).
[3]
Open Targets Platform — Drug–disease associations for Sapanisertib. EMBL-EBI & Wellcome Sanger Institute.
[4]
SEC EDGAR — Calithera Biosciences, Inc company filings. U.S. Securities and Exchange Commission.

Details

Drug Info

Quick Facts

Mechanism of Action: Serine/threonine-Protein Kinase MTOR Inhibitor[2]
Modality: Small molecule[2]
Highest Phase: Phase 2[1]
Company: CCalithera Biosciences, Inc

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