The importance of tracking “missing” metabolites: how and why?
S Wang, TE Ballard, LJ Christopher… - Journal of Medicinal …, 2023 - ACS Publications
Technologies currently employed to find and identify drug metabolites in complex biological
matrices generally yield results that offer a comprehensive picture of the drug metabolite …
matrices generally yield results that offer a comprehensive picture of the drug metabolite …
Designing out PXR activity on drug discovery projects: a review of structure-based methods, empirical and computational approaches
A Hall, H Chanteux, K Ménochet… - Journal of Medicinal …, 2021 - ACS Publications
This perspective discusses the role of pregnane xenobiotic receptor (PXR) in drug discovery
and the impact of its activation on CYP3A4 induction. The use of structural biology to reduce …
and the impact of its activation on CYP3A4 induction. The use of structural biology to reduce …
Pharmacokinetics and disposition of momelotinib revealed a disproportionate human metabolite—resolution for clinical development
J Zheng, Y Xin, J Zhang, R Subramanian… - Drug Metabolism and …, 2018 - ASPET
Momelotinib (MMB), a small-molecule inhibitor of Janus kinase (JAK) 1/2 and of activin A
receptor type 1 (ACVR1), is in clinical development for the treatment of myeloproliferative …
receptor type 1 (ACVR1), is in clinical development for the treatment of myeloproliferative …
Radiolabel uncovers nonintuitive metabolites of AMPAR potentiator BIIB104: Novel release of [14C] cyanide from 2-cyanothiophene and subsequent formation of [14C …
C Gu, J Huang, C Muste, J Zhong, GS Walker… - Drug Metabolism and …, 2024 - ASPET
BIIB104 (formerly PF-04958242), N-((3S, 4S)-4-(4-(5-cyanothiophen-2-yl) phenoxy)
tetrahydrofuran-3-yl) propane-2-sulfonamide, is an AMPAR potentiator investigated for the …
tetrahydrofuran-3-yl) propane-2-sulfonamide, is an AMPAR potentiator investigated for the …
The past decade of Genentech experience in elucidation of novel reaction mechanisms in drug metabolism
Drug metabolism is critical to many aspects of drug safety and efficacy. Thus, understanding
the various intricacies of drug metabolism helps to avoid possible pitfalls and contributes to …
the various intricacies of drug metabolism helps to avoid possible pitfalls and contributes to …
Investigation of the absolute bioavailability and human mass balance of navoximod, a novel IDO1 inhibitor
Aims Navoximod (GDC‐0919, NLG‐919) is a small molecule inhibitor of indoleamine‐2, 3‐
dioxygenase 1 (IDO1), developed to treat the acquired immune tolerance associated with …
dioxygenase 1 (IDO1), developed to treat the acquired immune tolerance associated with …
Perspective on the use of DNA repair inhibitors as a tool for imaging and radionuclide therapy of glioblastoma
L Everix, S Nair, CHS Driver, I Goethals, MM Sathekge… - Cancers, 2022 - mdpi.com
Simple Summary The current routine treatment for glioblastoma (GB), the most lethal high-
grade brain tumor in adults, aims to induce DNA damage in the tumor. However, the tumor …
grade brain tumor in adults, aims to induce DNA damage in the tumor. However, the tumor …
Late-occurring and long-circulating metabolites of GABAAα2, 3 receptor modulator AZD7325 involving metabolic cyclization and aromatization: Relevance to MIST …
AZD7325 [4-amino-8-(2-fluoro-6-methoxyphenyl)-N-propylcinnoline-3-carboxamide] is a
selective GABAA α 2, 3 receptor modulator intended for the treatment of anxiety disorders …
selective GABAA α 2, 3 receptor modulator intended for the treatment of anxiety disorders …
Radiolabel Uncovers Nonintuitive Metabolites of BIIB104: Novel Release of [14C] Cyanide from 2-Cyanothiophene and Subsequent Formation of [14C] Thiocyanate
C Gu, J Huang, C Muste, J Zhong, GS Walker… - Drug Metabolism and …, 2024 - ASPET
BIIB104 (formerly PF-04958242), N-((3 S, 4 S)-4-(4-(5-cyanothiophen-2-yl) phenoxy)
tetrahydrofuran-3-yl) propane-2-sulfonamide, is an α-amino-3-hydroxy-5-methyl-4 …
tetrahydrofuran-3-yl) propane-2-sulfonamide, is an α-amino-3-hydroxy-5-methyl-4 …
Mass Balance of the Indoleamine 2, 3‐Dioxygenase Inhibitor Navoximod (GDC-0919) in Rats and Dogs: Unexpected Cyanide Release from Imidazo [5, 1-a] isoindole …
Navoximod (GDC-0919) is a small molecule inhibitor of indoleamine 2, 3‐dioxygenase 1
(IDO1) developed to reduce T cell immunosuppression associated with cancer. This study …
(IDO1) developed to reduce T cell immunosuppression associated with cancer. This study …