Therapy Detail
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| Therapy Name | Sapanisertib |
| Synonyms | |
| Therapy Description |
Sapanisertib (MLN0128) is an ATP-competitive mTOR kinase inhibitor that induces apoptosis and inhibits growth in tumor cells (PMID: 25519700, PMID: 32488989). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Sapanisertib | INK128|INK-128|TAK-228|MLN0128|MLN-0128 | mTOR Inhibitor 51 | Sapanisertib (MLN0128) is an ATP-competitive mTOR kinase inhibitor that induces apoptosis and inhibits growth in tumor cells (PMID: 25519700, PMID: 32488989). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| PIK3CA mutant | Advanced Solid Tumor | sensitive | Sapanisertib | Preclinical | Actionable | In a preclinical study, human cancer cell lines harboring PIK3CA mutations were sensitive to Sapanisertib (MLN0128) as demonstrated by significant growth inhibition (PMID: 25261369). | 25261369 |
| PTEN mutant | breast cancer | sensitive | Sapanisertib | Preclinical | Actionable | In a preclinical study, Sapanisertib (MLN0128) induced apoptosis and inhibited MTORC1 signaling in breast cancer cells harboring a PTEN mutation (PMID: 25261369). | 25261369 |
| TSC1 inact mut | transitional cell carcinoma | no benefit | Sapanisertib | Phase II | Actionable | In a Phase II trial, treatment with Sapanisertib (MLN0128) in metastatic urothelial carcinoma patients with either a TSC1 or TSC2 activating mutation (n=13) did not result in an objective response and led to a median overall survival of 3.4 months, and the trial was terminated early due to limited clinical activity and poor drug tolerability (Journal of Clinical Oncology 39, no. 6_suppl (February 20, 2021) 431-431; NCT03047213). | detail... |
| TSC2 inact mut | transitional cell carcinoma | no benefit | Sapanisertib | Phase II | Actionable | In a Phase II trial, treatment with Sapanisertib (MLN0128) in metastatic urothelial carcinoma patients with either a TSC1 or TSC2 activating mutation (n=13) did not result in an objective response and led to a median overall survival of 3.4 months, and the trial was terminated early due to limited clinical activity and poor drug tolerability (Journal of Clinical Oncology 39, no. 6_suppl (February 20, 2021) 431-431; NCT03047213). | detail... |
| CDKN2A mut PIK3CA mut | breast cancer | sensitive | Sapanisertib | Preclinical | Actionable | In a preclinical study, a breast cancer cell line harboring mutations in PIK3CA and CDKN2A demonstrated sensitivity to Sapanisertib (MLN0128) in culture (PMID: 25261369). | 25261369 |
| PIK3CA mutant | breast cancer | sensitive | Sapanisertib | Preclinical | Actionable | In a preclinical study, Sapanisertib (MLN0128) demonstrated efficacy in PIK3CA mutant breast cancer xenograft models (PMID: 23085766). | 23085766 |
| PTEN mut TP53 mut | skin cancer | sensitive | Sapanisertib | Preclinical | Actionable | In a preclinical study, a skin cancer cell line harboring mutations in PTEN and TP53 demonstrated sensitivity to Sapanisertib (MLN0128) in culture (PMID: 25261369). | 25261369 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT01058707 | Phase I | Sapanisertib | Dose Escalation Study of MLN0128 in Subjects With Advanced Malignancies | Completed | USA | ESP | 0 |
| NCT02091531 | Phase II | Sapanisertib | Dual mTOR Inhibitor MLN0128 in Advanced Castration-Resistant Prostate Cancer (CRPC) Patients | Completed | USA | 0 |
| NCT02987959 | Phase II | Sapanisertib | Study of TAK-228 (MLN0128) in Soft Tissue Sarcomas | Terminated | USA | 0 |
| NCT02412722 | Phase I | Sapanisertib Paclitaxel | Safety, Tolerability, and Pharmacokinetics of MLN0128 as a Single Agent and in Combination With Paclitaxel in Adults With Advanced Nonhematologic Malignancies | Completed | USA | 0 |
| NCT02197572 | Phase I | Sapanisertib | Effect of MLN0128 on the QTc Interval in Participants With Advanced Solid Tumors | Completed | USA | 0 |
| NCT02725268 | Phase II | Paclitaxel Sapanisertib Sapanisertib + Serabelisib | Phase 2 Study of MLN0128, Combination of MLN0128 With MLN1117, Paclitaxel and Combination of MLN0128 With Paclitaxel in Women With Endometrial Cancer | Completed | USA | NOR | NLD | ITA | GBR | ESP | DEU | CAN | BEL | AUS | 0 |
| NCT02601209 | Phase Ib/II | Pazopanib Sapanisertib | Sapanisertib or Pazopanib Hydrochloride in Treating Patients With Locally Advanced or Metastatic Sarcoma | Terminated | USA | 0 |
| NCT03097328 | Phase II | Sapanisertib | Study of TAK-228 In Patients With Previously Treated Metastatic Renal Cell Carcinoma | Completed | USA | 0 |
| NCT02417701 | Phase II | Sapanisertib | Sapanisertib in Treating Patients With Stage IV or Recurrent Lung Cancer | Completed | USA | 0 |
| NCT02619669 | Phase I | Sapanisertib Letrozole | Neoadjuvant Run-In Study With TAK-228 (MLN0128) Followed by Letrozole/TAK-228 (MLN0128) in Women With High-Risk ER+/HER2- Breast Cancer | Withdrawn | USA | 0 |
| NCT02133183 | Phase I | Sapanisertib | TORC1/2 Inhibitor INK128 Before and After Surgery in Treating Patients With Recurrent Glioblastoma | Terminated | USA | 0 |
| NCT02484430 | Phase II | Sapanisertib | TORC1/2 Inhibitor INK128 in Treating Patients With Relapsed and/or Refractory Acute Lymphoblastic Leukemia | Active, not recruiting | USA | 0 |
| NCT02893930 | Phase II | Sapanisertib | Sapanisertib in Treating Patients With Metastatic or Refractory Pancreatic Neuroendocrine Tumor That Cannot Be Removed by Surgery | Completed | USA | 0 |
| NCT03047213 | Phase II | Sapanisertib | Sapanisertib in Treating Patients With Locally Advanced or Metastatic Bladder Cancer With TSC1 and/or TSC2 Mutations | Active, not recruiting | USA | 0 |
| NCT02514824 | Phase Ib/II | Sapanisertib | MLN0128 in Recurrent/Metastatic Merkel Cell Carcinoma | Completed | USA | 0 |
| NCT02724020 | Phase II | Sapanisertib + Serabelisib Sapanisertib Everolimus | MLN0128 and MLN0128 + MLN1117 Compared With Everolimus in the Treatment of Adults With Advanced or Metastatic Clear-Cell Renal Cell Carcinoma | Completed | USA | POL | ITA | GBR | FRA | ESP | CZE | CAN | 0 |
| NCT02575339 | Phase Ib/II | Sorafenib Sapanisertib | MLN0128 Compared to Sorafenib in Advanced or Metastatic Hepatocellular Carcinoma | Terminated | USA | 0 |
| NCT05275673 | Phase II | Sapanisertib | A Study of Sapanisertib in Relapsed/Refractory NFE2L2-Mutated and Wild-Type Squamous Non-Small Cell Lung Cancer | Terminated | USA | 0 |
| NCT02244463 | Phase II | Sapanisertib | A Phase II Study of MLN0128 in Metastatic Anaplastic Thyroid Cancer | Completed | USA | 0 |
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