sapanisertib

an mTOR inhibitor

Also Known As:

2-benzoxazolamine, 5-(4-amino-1-(1-methylethyl)-1H-pyrazolo(3,4-d)pyrimidin-3-yl)-; 3-(2-amino-1,3-benzoxazol-5-yl)-1-isopropyl-1H-pyrazolo(3,4-d)pyrimidin-4-amine; CB-228; INK128; MLN-0128; MLN0128; TAK-228

Networked: 99 relevant articles (13 outcomes, 40 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- Fused-Ring Heterocyclic Compounds
  - 2-Ring Heterocyclic Compounds
    - Purines: 651
      - Adenine: 2120
        sapanisertib: 99
    - Benzoxazoles: 68
      - sapanisertib: 99

Experts

1.	Neuwirth, Rachel: 4 articles (01/2022 - 06/2016)
2.	Calvisi, Diego F: 4 articles (10/2021 - 12/2017)
3.	Chen, Xin: 4 articles (10/2021 - 12/2017)
4.	Evert, Matthias: 4 articles (10/2021 - 12/2017)
5.	Shi, Guoping: 4 articles (01/2020 - 09/2018)
6.	Shokat, Kevan M: 4 articles (01/2020 - 02/2012)
7.	Faller, Douglas V: 3 articles (05/2022 - 11/2020)
8.	Sedarati, Farhad: 3 articles (05/2022 - 11/2020)
9.	Deming, Dustin A: 3 articles (01/2022 - 01/2019)
10.	Song, Xinhua: 3 articles (10/2021 - 12/2017)

Related Diseases

1.	Neoplasms (Cancer) 09/30/2014 - "Our results demonstrate that MLN0128 may be effective in tumors with intrinsic as well as acquired rapalog resistance. " 12/01/2017 - "MLN0128, a second generation pan-mTOR inhibitor, shows efficacy for multiple tumor types. " 05/01/2022 - "Correction to: A Phase 1 Study of Sapanisertib (TAK-228) in East Asian Patients with Advanced Nonhematological Malignancies." 01/01/2022 - "In this dose-escalation and expansion study, East Asian patients with nonhematologic malignancies received increasing sapanisertib doses once-daily (QD; starting at 2 mg) or once-weekly (QW; starting at 20 mg) in 28-day cycles. " 01/01/2022 - "A Phase 1 Study of Sapanisertib (TAK-228) in East Asian Patients with Advanced Nonhematological Malignancies."
2.	Breast Neoplasms (Breast Cancer) 12/01/2012 - "MLN0128 potently inhibited cell proliferation in various breast cancer cell lines harboring PIK3CA (IC(50): 1.5-53 nM), PTEN (IC(50): 1-149 nM), KRAS, and/or BRAF mutations (IC(50): 13-162 nM), and in human endothelial cells (IC(50): 33-40 nM) in vitro. " 12/01/2012 - "We assessed in vitro antiproliferative activity of MLN0128 in a panel of breast cancer cell lines. " 12/01/2012 - "Our findings support the clinical research of MLN0128 in patients with breast cancer and metastasis." 01/01/2022 - "Fulvestrant plus sapanisertib daily/weekly resulted in numerically longer PFS in patients with ER+/HER2- advanced or metastatic breast cancer, compared with single-agent fulvestrant. " 08/01/2018 - "Use of dual mTOR inhibitor MLN0128 against everolimus-resistant breast cancer."
3.	Renal Cell Carcinoma (Grawitz Tumor) 01/01/2022 - "In this multicenter, single-arm phase II trial, we evaluated the efficacy of sapanisertib in patients with treatment-refractory metastatic renal cell carcinoma (mRCC; NCT03097328). " 05/15/2014 - "Preclinical trial of a new dual mTOR inhibitor, MLN0128, using renal cell carcinoma tumorgrafts." 11/01/2020 - "In expansion cohorts, 82 patients with renal cell carcinoma (RCC), endometrial or bladder cancer received sapanisertib 5 mg QD (39 patients), 40 mg QW (26 patients) or 30 mg QW (17 patients). " 01/01/2022 - "Biomarker-Based Phase II Study of Sapanisertib (TAK-228): An mTORC1/2 Inhibitor in Patients With Refractory Metastatic Renal Cell Carcinoma." 12/09/2022 - "This phase II study evaluated the efficacy and safety of single-agent sapanisertib and sapanisertib plus the PI3Kα inhibitor TAK-117, vs. everolimus in patients with advanced clear cell renal cell carcinoma (ccRCC) that had progressed on or after VEGF-targeted therapy. "
4.	Primitive Neuroectodermal Tumors (PNET) 01/01/2019 - "Sapanisertib suppresses TF expression and activity and reduces the growth of pNET tumors in vivo. " 12/01/2018 - "Our PDX-PNET model is the first available, validated PDX model for PNET, and preclinical data from the use of this model suggest that sapanisertib may be an effective new treatment option for patients with PNET or everolimus-resistant PNET." 01/01/2019 - "Thus, further studies are warranted to evaluate the clinical utility of TF-suppressing mTORC1/2 inhibitor sapanisertib in pNET management." 12/01/2018 - "Treatment of PDX-PNETs with either everolimus or sapanisertib strongly inhibited growth. " 12/01/2022 - "A phase II study of sapanisertib (TAK-228) a mTORC1/2 inhibitor in rapalog-resistant advanced pancreatic neuroendocrine tumors (PNET): ECOG-ACRIN EA2161."
5.	Urinary Bladder Neoplasms (Bladder Cancer) 11/01/2020 - "In expansion cohorts, 82 patients with renal cell carcinoma (RCC), endometrial or bladder cancer received sapanisertib 5 mg QD (39 patients), 40 mg QW (26 patients) or 30 mg QW (17 patients). " 01/01/2019 - "TAK-228 is a promising investigational agent that induces a strong effect on cell proliferation, tumor growth, and angiogenesis in bladder cancer models. " 01/01/2019 - "TAK-228 also showed ex vivo activity in tumor tissue from patients with treatment-naïve bladder cancer. " 01/01/2019 - "A phase II study at our institution is currently evaluating the efficacy of TAK-228 combined with paclitaxel in patients with metastatic bladder cancer." 11/01/2020 - "Phase 1 study of mTORC1/2 inhibitor sapanisertib (TAK-228) in advanced solid tumours, with an expansion phase in renal, endometrial or bladder cancer."

Related Drugs and Biologics

1.	Mechanistic Target of Rapamycin Complex 1
2.	sapanisertib
3.	Paclitaxel (Taxol)
4.	Phosphotransferases (Kinase)
5.	MTOR Inhibitors
6.	Everolimus
7.	Tamoxifen
8.	Retinaldehyde (Retinal)
9.	Indicators and Reagents (Reagents)
10.	Ribosomal DNA (rDNA)

Related Therapies and Procedures

1.	Therapeutics
2.	Neoadjuvant Therapy
3.	Drug Therapy (Chemotherapy)
4.	Castration
5.	Stem Cell Transplantation