Inhibition of #CYP3A4 by #voriconazole
Voriconazole is potent inhibitor of CYP3A4. Tacrolimus is extensively metabolized by CYP3A4. When given together, voriconazole inhibits metabolism of tacrolimus, resulting in significantly ⬆️tacrolimus concentrations & ⬆️risk of nephrotoxicity & neurotoxicity.
【Research】
A double-humanized CYP3A4/PXR rat model was developed to better predict human drug–drug interactions.
This model holds promise for preclinical drug development pipelines.
Kobayashi et al 2025 PMID: 40721555
#CYP3A4 #PXR #HumanizedRat #Preclinical
【ラット研究紹介】CYP3A4とPXRをヒト化した「ダブルヒューマナイズドラット」薬物代謝や相互作用の予測に有用で、前臨床段階の創薬パイプラインへの応用に期待
Kobayashi et al 2025 PMID: 40721555
#創薬 #薬物動体 #CYP3A4 #PXR
Throwback to 2011: our lab investigated stereo- and chemoselective oxidations with Cytochrome P450, using an inexpensive chemical auxiliary. #chemsky #CYP3A4
pubs.acs.org/doi/10.1021/...
Grapefruit tastes even better than I remembered. I nearly cried it was so good. #TamoxifenVacation #BCSM #CYP3A4 @thankscancer.bsky.social
Every year in Nov/Dec when I start eating Clementines my tacrolimus (Prograf) trough levels "happen" to increase substantially (double..) if I've eaten a couple the day before the test. I'm convinced of #CYP3A4 link but I'm always told not.. any thoughts ?! www.vidal.fr/actualites/2... #nephsky
Why is everyone suddenly tweeting about the grapefruit juice effect? I was taught it in 1998. Has something changed? #CYP3A4