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The radiosensitizer Onalespib increases complete remission in (177)Lu-DOTATATE-treated mice bearing neuroendocrine tumor xenografts.
Lundsten S, Spiegelberg D, Raval NR, Nestor M. Lundsten S, et al. Eur J Nucl Med Mol Imaging. 2020 Apr;47(4):980-990. doi: 10.1007/s00259-019-04673-1. Epub 2020 Jan 7. Eur J Nucl Med Mol Imaging. 2020. PMID: 31912256 Free PMC article.
RESULTS: Biodistribution and autoradiography confirmed the SSTR-selective tumor uptake of (177)Lu-DOTATATE, which was unaffected by Onalespib treatment. Immunohistochemistry verified molecular responses to Onalespib therapy in the tumors. ...The damage was decreased …
RESULTS: Biodistribution and autoradiography confirmed the SSTR-selective tumor uptake of (177)Lu-DOTATATE, which was unaffected by Onale …
Phase Ib study of HSP90 inhibitor, onalespib (AT13387), in combination with paclitaxel in patients with advanced triple-negative breast cancer.
Williams NO, Quiroga D, Johnson C, Brufsky A, Chambers M, Bhattacharya S, Patterson M, Sardesai SD, Stover D, Lustberg M, Noonan AM, Cherian M, Bystry DM, Hill KL, Chen M, Phelps MA, Grever M, Stephens JA, Ramaswamy B, Carson WE 3rd, Wesolowski R. Williams NO, et al. Ther Adv Med Oncol. 2023 Dec 25;15:17588359231217976. doi: 10.1177/17588359231217976. eCollection 2023. Ther Adv Med Oncol. 2023. PMID: 38152697 Free PMC article.
Median DOR was 5.6 months; median PFS was 2.9 months. CONCLUSION: Combination treatment with onalespib and paclitaxel had an acceptable toxicity profile and RP2D was determined to be 260 mg/m(2) of onalespib. ...Despite minor drug-drug interactions between these 2 a …
Median DOR was 5.6 months; median PFS was 2.9 months. CONCLUSION: Combination treatment with onalespib and paclitaxel had an acceptab …
Combination therapy of tyrosine kinase inhibitor sorafenib with the HSP90 inhibitor onalespib as a novel treatment regimen for thyroid cancer.
Mortensen ACL, Berglund H, Hariri M, Papalanis E, Malmberg C, Spiegelberg D. Mortensen ACL, et al. Sci Rep. 2023 Oct 6;13(1):16844. doi: 10.1038/s41598-023-43486-z. Sci Rep. 2023. PMID: 37803074 Free PMC article.
This study examines enhancing sorafenib efficacy by combination therapy with the novel HSP90 inhibitor onalespib. In vitro efficacy of sorafenib and onalespib monotherapy as well as in combination was assessed in papillary (PTC) and anaplastic (ATC) thyroid cancer c …
This study examines enhancing sorafenib efficacy by combination therapy with the novel HSP90 inhibitor onalespib. In vitro efficacy o …
The HSP90 inhibitor onalespib potentiates 177Lu-DOTATATE therapy in neuroendocrine tumor cells.
Lundsten S, Spiegelberg D, Stenerlöw B, Nestor M. Lundsten S, et al. Int J Oncol. 2019 Dec;55(6):1287-1295. doi: 10.3892/ijo.2019.4888. Epub 2019 Sep 30. Int J Oncol. 2019. PMID: 31638190 Free PMC article.
Furthermore, onalespib was able to synergistically potentiate 177Lu-DOTATATE treatment in a SSTR-specific manner. The radiosensitizing mechanisms of onalespib involved the downregulation of EGFR expression and the induction of apoptosis. ...
Furthermore, onalespib was able to synergistically potentiate 177Lu-DOTATATE treatment in a SSTR-specific manner. The radiosensitizin …
Erlotinib and Onalespib Lactate Focused on EGFR Exon 20 Insertion Non-Small Cell Lung Cancer (NSCLC): A California Cancer Consortium Phase I/II Trial (NCI 9878).
Riess JW, Reckamp KL, Frankel P, Longmate J, Kelly KA, Gandara DR, Weipert CM, Raymond VM, Keer HN, Mack PC, Newman EM, Lara PN Jr. Riess JW, et al. Clin Lung Cancer. 2021 Nov;22(6):541-548. doi: 10.1016/j.cllc.2021.05.001. Epub 2021 May 15. Clin Lung Cancer. 2021. PMID: 34140248 Free PMC article. Clinical Trial.
BACKGROUND: Onalespib is a novel heat shock protein 90 inhibitor (HSP90i). Previous preclinical and clinical studies with HSP90i have demonstrated activity in EGFR-mutant non-small cell lung cancer (NSCLC). ...The recommended phase II dose is DL -1 (minus): erlotinib 150 m …
BACKGROUND: Onalespib is a novel heat shock protein 90 inhibitor (HSP90i). Previous preclinical and clinical studies with HSP90i have …
The HSP90 inhibitor Onalespib exerts synergistic anti-cancer effects when combined with radiotherapy: an in vitro and in vivo approach.
Spiegelberg D, Abramenkovs A, Mortensen ACL, Lundsten S, Nestor M, Stenerlöw B. Spiegelberg D, et al. Sci Rep. 2020 Apr 3;10(1):5923. doi: 10.1038/s41598-020-62293-4. Sci Rep. 2020. PMID: 32246062 Free PMC article.
Onalespib downregulated client proteins, lead to increased apoptosis and caused DNA-double-strands. ...In vivo, a minimal treatment regimen for 3 consecutive days of Onalespib (3 10 mg/kg) doubled survival, whereas Onalespib with radiotherapy (3 2 Gy) caused …
Onalespib downregulated client proteins, lead to increased apoptosis and caused DNA-double-strands. ...In vivo, a minimal treatment r …
Phase 1 study of the HSP90 inhibitor onalespib in combination with AT7519, a pan-CDK inhibitor, in patients with advanced solid tumors.
Do KT, O'Sullivan Coyne G, Hays JL, Supko JG, Liu SV, Beebe K, Neckers L, Trepel JB, Lee MJ, Smyth T, Gannon C, Hedglin J, Muzikansky A, Campos S, Lyons J, Ivy P, Doroshow JH, Chen AP, Shapiro GI. Do KT, et al. Cancer Chemother Pharmacol. 2020 Dec;86(6):815-827. doi: 10.1007/s00280-020-04176-z. Epub 2020 Oct 23. Cancer Chemother Pharmacol. 2020. PMID: 33095286 Free PMC article. Clinical Trial.
METHODS: This study followed a 3 + 3 trial design with 1 week of intravenous (IV) onalespib alone, followed by onalespib/AT7519 (IV) on days 1, 4, 8, and 11 of a 21-days cycle. ...There were no clinically relevant PK interactions for either drug. CONCLUSIONS: Combin …
METHODS: This study followed a 3 + 3 trial design with 1 week of intravenous (IV) onalespib alone, followed by onalespib/AT751 …
Efficacy of Onalespib, a Long-Acting Second-Generation HSP90 Inhibitor, as a Single Agent and in Combination with Temozolomide against Malignant Gliomas.
Canella A, Welker AM, Yoo JY, Xu J, Abas FS, Kesanakurti D, Nagarajan P, Beattie CE, Sulman EP, Liu J, Gumin J, Lang FF, Gurcan MN, Kaur B, Sampath D, Puduvalli VK. Canella A, et al. Clin Cancer Res. 2017 Oct 15;23(20):6215-6226. doi: 10.1158/1078-0432.CCR-16-3151. Epub 2017 Jul 5. Clin Cancer Res. 2017. PMID: 28679777 Free PMC article.
Brain and plasma pharmacokinetics of onalespib and its ability to inhibit HSP90 in vivo were assessed in non-tumor-bearing mice. ...Onalespib effectively crossed the BBB to inhibit HSP90 in vivo and extended survival as a single agent in zebrafish xenografts and in …
Brain and plasma pharmacokinetics of onalespib and its ability to inhibit HSP90 in vivo were assessed in non-tumor-bearing mice. ... …
Disruption of DNA Repair and Survival Pathways through Heat Shock Protein Inhibition by Onalespib to Sensitize Malignant Gliomas to Chemoradiation Therapy.
Xu J, Wu PJ, Lai TH, Sharma P, Canella A, Welker AM, Beattie CE, Elder JB, Easley M, Lonser R, Jacob NK, Pietrzak M, Timmers CM, Lang F, Sampath D, Puduvalli VK. Xu J, et al. Clin Cancer Res. 2022 May 2;28(9):1979-1990. doi: 10.1158/1078-0432.CCR-20-0468. Clin Cancer Res. 2022. PMID: 35140124 Free PMC article.
We evaluated whether compromising HR by targeting HSP90, a molecular chaperone required for the function of key HR proteins, using onalespib, a long-acting, brain-penetrant HSP90 inhibitor, would sensitize high-grade gliomas to chemoradiation in vitro and in vivo. ...HSP90 …
We evaluated whether compromising HR by targeting HSP90, a molecular chaperone required for the function of key HR proteins, using onales …
61 results