Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation

Search Page

Filters

My NCBI Filters

Results by year

Table representation of search results timeline featuring number of search results per year.

Year Number of Results
2021 1
2022 2
2023 8
2024 3

Text availability

Article attribute

Article type

Publication date

Search Results

13 results

Results by year

Filters applied: . Clear all
Page 1
Did you mean acalisib (2 results)?
Just a spoonful of metformin helps the medicine go down.
Tzaridis T, Wechsler-Reya RJ. Tzaridis T, et al. J Clin Invest. 2024 Mar 15;134(6):e179144. doi: 10.1172/JCI179144. J Clin Invest. 2024. PMID: 38488006 Free PMC article.
After identifying the PI3K/mTOR pathway as a therapeutic vulnerability, they treated DIPG-bearing mice with paxalisib and saw responses but also observed hyperglycemia as a severe side effect. Combining paxalisib with metformin mitigated this toxicity, but also upre …
After identifying the PI3K/mTOR pathway as a therapeutic vulnerability, they treated DIPG-bearing mice with paxalisib and saw respons …
PI3K/mTOR is a therapeutically targetable genetic dependency in diffuse intrinsic pontine glioma.
Duchatel RJ, Jackson ER, Parackal SG, Kiltschewskij D, Findlay IJ, Mannan A, Staudt DE, Thomas BC, Germon ZP, Laternser S, Kearney PS, Jamaluddin MFB, Douglas AM, Beitaki T, McEwen HP, Persson ML, Hocke EA, Jain V, Aksu M, Manning EE, Murray HC, Verrills NM, Sun CX, Daniel P, Vilain RE, Skerrett-Byrne DA, Nixon B, Hua S, de Bock CE, Colino-Sanguino Y, Valdes-Mora F, Tsoli M, Ziegler DS, Cairns MJ, Raabe EH, Vitanza NA, Hulleman E, Phoenix TN, Koschmann C, Alvaro F, Dayas CV, Tinkle CL, Wheeler H, Whittle JR, Eisenstat DD, Firestein R, Mueller S, Valvi S, Hansford JR, Ashley DM, Gregory SG, Kilburn LB, Nazarian J, Cain JE, Dun MD. Duchatel RJ, et al. J Clin Invest. 2024 Feb 6;134(6):e170329. doi: 10.1172/JCI170329. J Clin Invest. 2024. PMID: 38319732 Free PMC article.
Analysis of CRISPR/Cas9 loss-of-function gene deletion screens identified PIK3CA and MTOR as targetable molecular dependencies across patient derived models of DIPG, highlighting the therapeutic potential of the blood-brain barrier-penetrant PI3K/Akt/mTOR inhibitor, paxalisib …
Analysis of CRISPR/Cas9 loss-of-function gene deletion screens identified PIK3CA and MTOR as targetable molecular dependencies across patien …
Preclinical characterization of the absorption and disposition of the brain penetrant PI3K/mTOR inhibitor paxalisib and prediction of its pharmacokinetics and efficacy in human.
Salphati L, Pang J, Alicke B, Plise EG, Cheong J, Jaochico A, Olivero AG, Sampath D, Wong S, Zhang X. Salphati L, et al. Xenobiotica. 2024 Feb;54(2):64-74. doi: 10.1080/00498254.2024.2303586. Epub 2024 Jan 15. Xenobiotica. 2024. PMID: 38197324
We characterised the preclinical pharmacokinetics and efficacy of paxalisib and predicted its pharmacokinetics and efficacious dose in humans.Plasma protein binding of paxalisib was low, with the fraction unbound ranging from 0.25 to 0.43 across species. The hepatic …
We characterised the preclinical pharmacokinetics and efficacy of paxalisib and predicted its pharmacokinetics and efficacious dose i …
Rational combination platform trial design for children and young adults with Diffuse Midline Glioma: a report from PNOC.
Mueller S, Kline C, Franson A, van der Lugt J, Prados M, Waszak SM, Plasschaert S, Molinaro AM, Koschmann C, Nazarian J. Mueller S, et al. Neuro Oncol. 2023 Dec 20:noad181. doi: 10.1093/neuonc/noad181. Online ahead of print. Neuro Oncol. 2023. PMID: 38124481
We have previously shown preclinical efficacy of targeting both oxidative phosphorylation and glycolysis through treatment with ONC201, which activates the mitochondrial protease ClpP, and paxalisib, which inhibits PI3K/mTOR, respectively. This combination treatment aimed …
We have previously shown preclinical efficacy of targeting both oxidative phosphorylation and glycolysis through treatment with ONC201, whic …
Enhanced Sestrin expression through Tanshinone 2A treatment improves PI3K-dependent inhibition of glioma growth.
Schaf J, Shinhmar S, Zeng Q, Pardo OE, Beesley P, Syed N, Williams RSB. Schaf J, et al. Cell Death Discov. 2023 May 19;9(1):172. doi: 10.1038/s41420-023-01462-6. Cell Death Discov. 2023. PMID: 37202382 Free PMC article.
We then translate our findings to human and mouse-derived glioblastoma cell lines, where both a PI3K inhibitor (Paxalisib) and T2A reduces glioblastoma proliferation in monolayer cultures and in spheroid expansion, with combinatory treatment significantly enhancing this ef …
We then translate our findings to human and mouse-derived glioblastoma cell lines, where both a PI3K inhibitor (Paxalisib) and T2A re …
ONC201 in Combination with Paxalisib for the Treatment of H3K27-Altered Diffuse Midline Glioma.
Jackson ER, Duchatel RJ, Staudt DE, Persson ML, Mannan A, Yadavilli S, Parackal S, Game S, Chong WC, Jayasekara WSN, Grand ML, Kearney PS, Douglas AM, Findlay IJ, Germon ZP, McEwen HP, Beitaki TS, Patabendige A, Skerrett-Byrne DA, Nixon B, Smith ND, Day B, Manoharan N, Nagabushan S, Hansford JR, Govender D, McCowage GB, Firestein R, Howlett M, Endersby R, Gottardo NG, Alvaro F, Waszak SM, Larsen MR, Colino-Sanguino Y, Valdes-Mora F, Rakotomalala A, Meignan S, Pasquier E, André N, Hulleman E, Eisenstat DD, Vitanza NA, Nazarian J, Koschmann C, Mueller S, Cain JE, Dun MD. Jackson ER, et al. Cancer Res. 2023 May 17:OF1-OF17. doi: 10.1158/0008-5472.CAN-23-0186. Online ahead of print. Cancer Res. 2023. PMID: 37195023
Metabolic adaptation and reduced sensitivity to ONC201 was promoted by redox-activated PI3K/Akt signaling, which could be counteracted using the brain penetrant PI3K/Akt inhibitor, paxalisib. Together, these discoveries coupled with the powerful anti-DIPG/DMG pharmacokinet …
Metabolic adaptation and reduced sensitivity to ONC201 was promoted by redox-activated PI3K/Akt signaling, which could be counteracted using …
ONC201 in combination with paxalisib for the treatment of H3K27-altered diffuse midline glioma.
Jackson ER, Duchatel RJ, Staudt DE, Persson ML, Mannan A, Yadavilli S, Parackal S, Game S, Chong WC, Jayasekara WSN, Le Grand M, Kearney PS, Douglas AM, Findlay IJ, Germon ZP, McEwen HP, Beitaki TS, Patabendige A, Skerrett-Byrne DA, Nixon B, Smith ND, Day B, Manoharan N, Nagabushan S, Hansford JR, Govender D, McCowage GB, Firestein R, Howlett M, Endersby R, Gottardo NG, Alvaro F, Waszak SM, Larsen MR, Colino-Sanguino Y, Valdés-Mora F, Rakotomalala A, Meignan S, Pasquier E, Andre N, Hulleman E, Eisenstat DD, Vitanza NA, Nazarian J, Koschmann C, Mueller S, Cain JE, Dun MD. Jackson ER, et al. Cancer Res. 2023 May 5;83(14):2421-37. doi: 10.1158/0008-5472.CAN-23-0186. Online ahead of print. Cancer Res. 2023. PMID: 37145169 Free PMC article.
Metabolic adaptation and reduced sensitivity to ONC201 was promoted by redox-activated PI3K/Akt signaling, which could be counteracted using the brain penetrant PI3K/Akt inhibitor, paxalisib. Together, these discoveries coupled with the powerful anti-DIPG/DMG pharmacokinet …
Metabolic adaptation and reduced sensitivity to ONC201 was promoted by redox-activated PI3K/Akt signaling, which could be counteracted using …
Validated liquid chromatography with tandem mass spectrometry method for determination of paxalisib in mouse plasma: An application to pharmacokinetic study in mice.
A B V, Das A. A B V, et al. Biomed Chromatogr. 2023 Aug;37(8):e5650. doi: 10.1002/bmc.5650. Epub 2023 May 2. Biomed Chromatogr. 2023. PMID: 37070164
Paxalisib was stable under a series of stability conditions. Post-oral administration to mice, paxalisib maximum plasma concentrations were attained at 2.0 h. Paxalisib's half-life ranged between 3.2 and 4.2 h. Paxalisib exhibited low clearance and mod …
Paxalisib was stable under a series of stability conditions. Post-oral administration to mice, paxalisib maximum plasma concen …
Validated HPLC-UV method for quantification of paxalisib, a pan PI3K and mTOR inhibitor in mouse plasma: Application to a pharmacokinetic study in mice.
Zakkula A, Tripathy HK, Bestha RM, Vinod AB, Kiran V, Dittakavi S, Mullangi R. Zakkula A, et al. Biomed Chromatogr. 2023 Apr;37(4):e5587. doi: 10.1002/bmc.5587. Epub 2023 Jan 30. Biomed Chromatogr. 2023. PMID: 36680551
Paxalisib is a pan-PI3K and mTOR inhibitor, currently entering into Phase II clinical trials as a potential drug to treat glioblastoma patients. ...The validated HPLC method was extended to assess the pharmacokinetic parameters of paxalisib in mice....
Paxalisib is a pan-PI3K and mTOR inhibitor, currently entering into Phase II clinical trials as a potential drug to treat glioblastom …
Real-time drug testing of paediatric diffuse midline glioma to support clinical decision making: The Zurich DIPG/DMG centre experience.
Mueller T, Laternser S, Guerreiro Stücklin AS, Gerber NU, Mourabit S, Rizo M, Rushing EJ, Kottke R, Grotzer M, Krayenbühl N, Nazarian J, Mueller S. Mueller T, et al. Eur J Cancer. 2023 Jan;178:171-179. doi: 10.1016/j.ejca.2022.10.014. Epub 2022 Oct 26. Eur J Cancer. 2023. PMID: 36455411
Genome and RNA expression were used to further guide treatment strategies with targeted agents such as dual PI3K/mTOR inhibitor paxalisib. CONCLUSION: We established a systematic workflow for safe, robot-assisted brainstem biopsies and in-house tissue processing, followed …
Genome and RNA expression were used to further guide treatment strategies with targeted agents such as dual PI3K/mTOR inhibitor paxalisib …
13 results