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Development of an enhanced formulation to minimize pharmacokinetic variabilities of a weakly basic drug compound

Autor: Yu (Elaine) Pu, Robert Menger, Zeen Tong, Tracy Gaebele

Publikováno v: Pharmaceutical development and technology. 27(4)

Formulating poorly water soluble, weakly basic drugs with consistent exposure is often a challenge due to pH-dependent solubility. When the oral formulation is exposed to different pH ranges in the gastrointestinal (GI) tract, drug precipitation, or

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e887210c857ade3cbad2bc032ed83ca4
https://pubmed.ncbi.nlm.nih.gov/35502986

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Assessment of Transporter-Mediated Drug Interactions for Enasidenib Based on a Cocktail Study in Patients With Relapse or Refractory Acute Myeloid Leukemia or Myelodysplastic Syndrome

Autor: Leon Carayannopoulos, Josephine Reyes, Xiaomin Wang, Yan Li, Simon Zhou, Yiming Cheng, Zeen Tong

Publikováno v: Journal of clinical pharmacologyReferences. 62(4)

As a first-in-class, selective, potent inhibitor of the isocitrate dehydrogenase-2 (IDH2) mutant protein, enasidenib was approved by the US Food and Drug Administration in 2017 for the treatment of adult patients with relapsed or refractory acute mye

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::19341653429c5b132c25eca396c2910c
https://pubmed.ncbi.nlm.nih.gov/34617279

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Modeling and simulation of the endogenous CYP3A induction marker 4β-hydroxycholesterol during enasidenib treatment

Autor: Maria Palmisano, Yan Li, Zeen Tong, Jamie N. Connarn, Jian Chen, Simon Zhou

Publikováno v: Clinical Pharmacology: Advances and Applications. 11:39-50

Background Enasidenib (IDHIFA®, AG-221) is a first-in-class, targeted inhibitor of mutant IDH2 proteins for treatment of relapsed or refractory acute myeloid leukemia. This was a Phase I/II study evaluating safety, efficacy, and pharmacokinetics/pha

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::2e49ed47315a0ebba9a868cd84c28c12
https://doi.org/10.2147/cpaa.s192687

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In vitro inhibition of human nucleoside transporters and uptake of azacitidine by an isocitrate dehydrogenase-2 inhibitor enasidenib and its metabolite AGI-16903

Autor: Zeen Tong, Matthew Hoffmann, James D. Young, Sylvia Y.M. Yao, Usha Yerramilli, Sekhar Surapaneni

Publikováno v: Xenobiotica. 49:1229-1236

1. The present study investigated inhibitory effects of enasidenib and its metabolite AGI-16903 on (a) recombinant human nucleoside transporters (hNTs) in hNT-producing Xenopus laevis oocytes, and ...

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ca44bea0c974d331ccc39c25defea606
https://doi.org/10.1080/00498254.2018.1539783

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Quantification of azacitidine incorporation into human DNA/RNA by accelerator mass spectrometry as direct measure of target engagement

Autor: Stephen E. Maxwell, Xiaomin Wang, Irene Nooijen, Wouter H. J. Vaes, Zeen Tong, Daniel Menezes, Esther van Duijn

Publikováno v: Journal of Pharmaceutical and Biomedical Analysis. 202:114152

We report an accelerator mass spectrometry (AMS) assay to quantify azacitidine (Aza) incorporation into DNA and RNA from human acute myeloid leukemia (AML) cells, mouse bone marrow (BM) and peripheral blood mononuclear cells (PBMCs). Aza, a cytidine

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::76420f56baee521689b8c61f24436457
https://doi.org/10.1016/j.jpba.2021.114152

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Modeling and simulation of the endogenous CYP3A induction marker 4β-hydroxycholesterol during enasidenib treatment

Autor: Yan, Li, Jamie N, Connarn, Jian, Chen, Zeen, Tong, Maria, Palmisano, Simon, Zhou

Publikováno v: Clinical Pharmacology : Advances and Applications

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::671499524f160c002a7050f30c94ebf7
https://pubmed.ncbi.nlm.nih.gov/30858735

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Superior therapeutic efficacy of nab-paclitaxel over cremophor-based paclitaxel in locally advanced and metastatic models of human pancreatic cancer

Autor: Shihe Hou, Shinichi Yabuuchi, Zeen Tong, Carla Heise, Daniel D. Von Hoff, Manuel Hidalgo, N. V. Rajeshkumar, Shweta G. Pai, Daniel W. Pierce, Anirban Maitra, Scott Bateman

Publikováno v: British Journal of Cancer

Background: Albumin-bound paclitaxel (nab-paclitaxel, nab-PTX) plus gemcitabine (GEM) combination has demonstrated efficient antitumour activity and statistically significant overall survival of patients with metastatic pancreatic ductal adenocarcino

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::71068e0e93b5a2d7cdfc6b348d6dacaf
https://doi.org/10.1038/bjc.2016.215

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Assessment of drug-drug interaction potential and PBPK modeling of CC-223, a potent inhibitor of the mammalian target of rapamycin kinase

Autor: Yan Li, Jim Nissel, Sekhar Surapaneni, Rangaraj Narayanan, Hong Liu, Christian Atsriku, Xiaomin Wang, Zeen Tong

Publikováno v: Xenobiotica; the fate of foreign compounds in biological systems. 49(1)

1. CC-223 was studied in vitro for metabolism and drug-drug interactions (DDI), and in clinic for interaction with ketoconazole. 2. In vitro, human metabolites of CC-223 included O-desmethyl CC-223 (M1), keto (M2), N-oxide (M3) and imine (M13), with

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::afef4248cd359e781f4071f3043cff4e
https://pubmed.ncbi.nlm.nih.gov/29297772

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