CYP3A5

Cletoquine 是 Hydroxychloroquine 的主要活性代谢物。 Cletoquine 具有对抗基孔肯雅病毒 (CHIKV) 的能力。 Cletoquine 具有抗疟作用，并具有治疗自身免疫性疾病的潜力。

PF-4981517 (CYP3cide) 是一种高效，特异性和时间依赖性细胞色素P4503A4 (CYP3A4)抑制剂。对于CYP3A4，CYP3A5 和 CYP3A7，抑制CYP3A 活性的IC50值分别为 0.03 μM，17 μM 和 71μM。PF-4981517 可用于区分CYP3A4和 CYP3A5 对于药物代谢的作用。

Clobetasol propionate (CGP9555) 是CYP3A5的选择性抑制剂(IC50:0.206 μM)，而对 CYP3A4 或其他主要 CYP 无抑制作用。它是皮质类固醇，对于牛皮癣和其他皮肤病具有潜在的研究价值。

N-Desethyl vardenafil is a metabolite of vardenafil , a phosphodiesterase 5 inhibitor, that is formed by the action of cytochrome P450 (CYP)3A4 and CYP3A5.

The naturally-occurring estrogens are estrone , estradiol , and estriol . 16α-hydroxy Estrone (16α-OHE1) is a hydroxylated metabolite of E1 as well as an interconversion product with E2. E1 is 16α-hydroxylated by cytochrome P450 (CYP) isoforms, including CYP1A1, CYP3A5, CYP3A4, and CYP3A7, with CYP3A5 being breast-specific. 16α-OHE1 is sulphatized or glucuronidated before excretion. It is increased in rheumatoid arthritis and decreased by physical activity. Unlike the parent estrogens and other hydroxylated metabolites of E1, 16α-OHE1 binds covalently and persistently activates estrogen receptors. In addition, this metabolite increases cell proliferation and does not suppress TNF-α secretion, whereas other estrogen metabolites are not pro-proliferative and have marked effects on TNF-α secretion. The levels of 16α-OHE1 are increased in some forms of hormone therapy. Because hormone therapy increases breast cancer risk, 16α-OHE1 has been implicated as a risk factor for breast cancer, although supportive data remains elusive.

N-Desmethyl sildenafil is a major metabolite of sildenafil . N-Desmethyl sildenafil is formed via oxidative metabolism of sildenafil by the cytochrome (CYP) P450 isoforms CYP3A4, CYP3A5, and CYP3A7.

(3S)-hydroxy Quinidine is an active quinidine metabolite. Quinidine, an antiarrhythmic agent, undergoes rapid first-pass metabolism by the cytochrome P450 (CYP) isoforms CYP3A4, CYP2C9, CYP2E1, and CYP3A5, with CYP3A4 being the most active enzyme in the (3S)-hydroxy quinidine formation. (3S)-hydroxy Quinidine prolongs repolarization of canine Purkinje fibers in vitro and prevents ventricular fibrillation and ventricular tachycardia after coronary reperfusion in isolated rat hearts in a dose-dependent manner.

Dehydro Nifedipine (BAY-b 4759) 是人血浆中硝苯地平的主要代谢物。Dehydro Nifedipine 抑制PC-12细胞葡萄糖摄取，IC50值为130 μM，硝苯地平是一种钙通道阻滞剂，用于治疗高血压和心绞痛。当硝苯地平被细胞色素P450 (CYP)异构体CYP3A4和CYP3A5代谢时形成脱氢硝苯地平。

6β-hydroxy Eplerenone is a major metabolite of the mineralocorticoid receptor antagonist eplerenone .1 It is formed from eplerenone by the cytochrome P450 (CYP) isoform CYP3A4. |1. Cook, C.S., Berry, L.M., Kim, D.H., et al. Involvement of CYP3A in the metabolism of eplerenone in humans and dogs: Differential metabolism by CYP3A4 and CYP3A5. Drug Metab. Dispos. 30(12), 1344-1351 (2002).

6β-Hydroxy Prednisolone, the active metabolite of prednisone and a derivative of prednisolone, is predominantly synthesized via the cytochrome P450 (CYP) isoform CYP3A4 and, to a lesser extent, CYP3A5.

Desethoxy quetiapine, an active metabolite of the atypical antipsychotic quetiapine, primarily forms through the action of the cytochrome P450 (CYP) isoform CYP3A5. This compound binds to dopamine D2 receptors with an IC50 value of 1,330 nM. In vivo, desethoxy quetiapine at dosages of 20 and 40 mg kg mitigates dopamine receptor agonist apomorphine-induced climbing behavior and ameliorates swimming deficits in mice, showcasing its potential modulatory effects on dopamine-mediated behaviors.