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Year Number of Results
2014 4
2015 1
2016 2
2017 2
2018 5
2019 3
2020 2
2021 6
2022 4
2023 4
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Page 1
Akt Pathway Inhibitors.
Uko NE, Güner OF, Matesic DF, Bowen JP. Uko NE, et al. Curr Top Med Chem. 2020;20(10):883-900. doi: 10.2174/1568026620666200224101808. Curr Top Med Chem. 2020. PMID: 32091335 Review.
There have been several promising drug candidates that have been studied, including but not limited to ipatasertib (RG7440), 1; afuresertib (GSK2110183), 2; uprosertib (GSK2141795), 3; capivasertib (AZD5363), 4; which reportedly bind to the ATP active site and inhibit Akt …
There have been several promising drug candidates that have been studied, including but not limited to ipatasertib (RG7440), 1; afuresert …
The Protective Mechanism of Afuresertib against Esophageal Cancer.
Min B, Wang Y, Liang F, Wang CX, Wang F, Yang Z. Min B, et al. Dis Markers. 2022 Jul 14;2022:1832241. doi: 10.1155/2022/1832241. eCollection 2022. Dis Markers. 2022. PMID: 35872696 Free PMC article.
In this study, we determined the effect of different concentrations of afuresertib on cell viability by MTT assay and determined the effect of afuresertib on cell apoptosis by Annexin V-FITC/PI dual staining. Animal experiments verified the effects of afuresertib …
In this study, we determined the effect of different concentrations of afuresertib on cell viability by MTT assay and determined the …
The novel AKT inhibitor afuresertib suppresses human Merkel cell carcinoma MKL-1 cell growth.
Wu JH, Limmer AL, Narayanan D, Doan HQ, Simonette RA, Rady PL, Tyring SK. Wu JH, et al. Clin Exp Dermatol. 2021 Dec;46(8):1551-1554. doi: 10.1111/ced.14798. Epub 2021 Aug 26. Clin Exp Dermatol. 2021. PMID: 34115902
In the current study, we found that AKT has important regulatory functions in MCC cells and that inhibition of AKT with the novel ATP-competitive AKT inhibitor, afuresertib, has widespread effects on proliferative pathways. In particular, we found that treatment of MCC cel …
In the current study, we found that AKT has important regulatory functions in MCC cells and that inhibition of AKT with the novel ATP-compet …
Novel ATP-competitive Akt inhibitor afuresertib suppresses the proliferation of malignant pleural mesothelioma cells.
Yamaji M, Ota A, Wahiduzzaman M, Karnan S, Hyodo T, Konishi H, Tsuzuki S, Hosokawa Y, Haniuda M. Yamaji M, et al. Cancer Med. 2017 Nov;6(11):2646-2659. doi: 10.1002/cam4.1179. Epub 2017 Sep 27. Cancer Med. 2017. PMID: 28960945 Free PMC article.
Furthermore, afuresertib significantly enhanced cisplatin-induced cytotoxicity. Interestingly, results of gene set enrichment analysis showed that afuresertib modulated the expression E2F1 and MYC, which are associated with fibroblast core serum response. Together, …
Furthermore, afuresertib significantly enhanced cisplatin-induced cytotoxicity. Interestingly, results of gene set enrichment analysi …
A phase IIa study of afuresertib, an oral pan-AKT inhibitor, in patients with Langerhans cell histiocytosis.
Arceci RJ, Allen CE, Dunkel IJ, Jacobsen E, Whitlock J, Vassallo R, Morris SR, Portnoy A, Reedy BA, Smith DA, Noble R, Murnane A, Cornfeld M, Rodriguez-Galindo C, Heaney ML, McClain K, Vaiselbuh S. Arceci RJ, et al. Pediatr Blood Cancer. 2017 May;64(5). doi: 10.1002/pbc.26325. Epub 2016 Nov 2. Pediatr Blood Cancer. 2017. PMID: 27804235 Clinical Trial.
A clinical response in an adult patient with LCH participating in the first-in-human trial of afuresertib prompted this prospective trial. PROCEDURE: The population in the current study included treatment-naive (n = 7) and recurrent/refractory patients with LCH (n = 10), w …
A clinical response in an adult patient with LCH participating in the first-in-human trial of afuresertib prompted this prospective t …
Phase IB Dose Escalation and Expansion Study of AKT Inhibitor Afuresertib with Carboplatin and Paclitaxel in Recurrent Platinum-resistant Ovarian Cancer.
Blagden SP, Hamilton AL, Mileshkin L, Wong S, Michael A, Hall M, Goh JC, Lisyanskaya AS, DeSilvio M, Frangou E, Stronach EA, Gopalakrishna P, Meniawy TM, Gabra H. Blagden SP, et al. Clin Cancer Res. 2019 Mar 1;25(5):1472-1478. doi: 10.1158/1078-0432.CCR-18-2277. Epub 2018 Dec 18. Clin Cancer Res. 2019. PMID: 30563934 Free article. Clinical Trial.
Three dose-limiting toxicities of grade 3 rash were observed, one at 125 mg and two at 150 mg afuresertib. The MTD of afuresertib in combination with PC was therefore identified as 125 mg/day. ...Median progression-free survival was 7.1 months (95% CI, 6.3-9.0 month …
Three dose-limiting toxicities of grade 3 rash were observed, one at 125 mg and two at 150 mg afuresertib. The MTD of afuresertib …
The novel AKT inhibitor afuresertib shows favorable safety, pharmacokinetics, and clinical activity in multiple myeloma.
Spencer A, Yoon SS, Harrison SJ, Morris SR, Smith DA, Brigandi RA, Gauvin J, Kumar R, Opalinska JB, Chen C. Spencer A, et al. Blood. 2014 Oct 2;124(14):2190-5. doi: 10.1182/blood-2014-03-559963. Epub 2014 Jul 29. Blood. 2014. PMID: 25075128 Free PMC article. Clinical Trial.
We conducted an open-label phase 1 study to evaluate the maximum tolerated dose (MTD), safety, pharmacokinetics, and clinical activity of afuresertib-an oral AKT inhibitor-in patients with advanced hematologic malignancies. ...Clinical activity was also observed in non-Hod …
We conducted an open-label phase 1 study to evaluate the maximum tolerated dose (MTD), safety, pharmacokinetics, and clinical activity of …
Azeliragon inhibits PAK1 and enhances the therapeutic efficacy of AKT inhibitors in pancreatic cancer.
Kong W, Zhu L, Li T, Chen J, Fan B, Ji W, Zhang C, Cai X, Hu C, Sun X, Cao P. Kong W, et al. Eur J Pharmacol. 2023 Jun 5;948:175703. doi: 10.1016/j.ejphar.2023.175703. Epub 2023 Apr 5. Eur J Pharmacol. 2023. PMID: 37028543
Azeliragon was also found to significantly inhibit tumor growth in a pancreatic cancer xenograft model; when combined with afuresertib, an oral pan-AKT kinase inhibitor, azeliragon exhibited a strong synergistic effect against pancreatic cancer cells. Interestingly, afu …
Azeliragon was also found to significantly inhibit tumor growth in a pancreatic cancer xenograft model; when combined with afuresertib …
A phase 2 study of ofatumumab (Arzerra()) in combination with a pan-AKT inhibitor (afuresertib) in previously treated patients with chronic lymphocytic leukemia (CLL).
Chen CI, Paul H, Le LW, Wei EN, Snitzler S, Wang T, Levina O, Kakar S, Lau A, Queau M, Johnston JB, Smith DA, Trudel S. Chen CI, et al. Leuk Lymphoma. 2019 Jan;60(1):92-100. doi: 10.1080/10428194.2018.1468892. Epub 2018 Jun 19. Leuk Lymphoma. 2019. PMID: 29916761 Clinical Trial.
In this phase 2 trial, 30 relapsed/refractory CLL patients were treated with combination afuresertib, a novel oral AKT inhibitor, and ofatumumab for 6 months, followed by afuresertib maintenance for 12 months. ...Median progression-free survival was 8.5 months and o …
In this phase 2 trial, 30 relapsed/refractory CLL patients were treated with combination afuresertib, a novel oral AKT inhibitor, and …
Phase I study of the MEK inhibitor trametinib in combination with the AKT inhibitor afuresertib in patients with solid tumors and multiple myeloma.
Tolcher AW, Patnaik A, Papadopoulos KP, Rasco DW, Becerra CR, Allred AJ, Orford K, Aktan G, Ferron-Brady G, Ibrahim N, Gauvin J, Motwani M, Cornfeld M. Tolcher AW, et al. Cancer Chemother Pharmacol. 2015 Jan;75(1):183-9. doi: 10.1007/s00280-014-2615-5. Epub 2014 Nov 25. Cancer Chemother Pharmacol. 2015. PMID: 25417902 Clinical Trial.
Dose-limiting toxicities (Grade 2 esophagitis; Grade 3 aspartate aminotransferase increased, mucosal inflammation and hypokalemia) were reported at starting dose (1.5 mg trametinib/50 mg afuresertib once daily continuously), exceeding the MTD. Subsequent de-escalation coho …
Dose-limiting toxicities (Grade 2 esophagitis; Grade 3 aspartate aminotransferase increased, mucosal inflammation and hypokalemia) were repo …
31 results