CYP-450

Itraconazole (R51211) is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes necessary for ERGOSTEROL synthesis.

Naringin (Naringoside), a flavanone glycoside, exerts various of pharmacological effects such as blood lipid lowering, antioxidant activity, anticancer activity, and inhibition of cytochrome P450 enzymes.

Levobupivacaine is an amino-amide local anaesthetic drug belonging to the family of n-alkylsubstituted pipecoloxylidide. It is the S-enantiomer of bupivacaine. Levobupivacaine hydrochloride is commonly marketed by AstraZeneca under the trade name Chirocaine. Compared to bupivacaine, levobupivacaine is associated with less vasodilation and has a longer duration of action. It is approximately 13 per cent less potent (by molarity) than racemic bupivacaine.Levobupivacaine is indicated for local anaesthesia including infiltration, nerve block, ophthalmic, epidural and intrathecal anaesthesia in adults; and infiltration analgesia in children. Adverse drug reactions (ADRs) are rare when it is administered correctly. Most ADRs relate to administration technique (resulting in systemic exposure) or pharmacological effects of anesthesia, however allergic reactions can rarely occur.

Danshensu sodium salt (Sodium Danshensu) is sodium salt of danshensu from the widely used Chinese herb Danshen. It can inhibited phenylephrine- and CaCl2-induced vasoconstriction in Ca2+-free medium.

Tetrahydropiperine (Cosmoperine) is a natural product derived from piperine, can be used to treat convulsion, epilepsy, relieve pain, and control insects.

1-Aminobenzotriazole (ABT) (ABT) is a non-specific cytochrome P450 (CYP) inhibitor.

Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a reversible neuronal sodium channel inhibitor and the pure S(-)-enantiomer of bupivacaine, used as a long-acting local anesthetic.

Quinidine sulfate dihydrate (Pitayine Sodium) is a potent and selective cytochrome P450db inhibitor

Liarozole (R75251 dihydrochloride) is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase).Liarozole dihydrochloride is an imidazole derivative; it is being investigated as a non-hormonal agent in prostate cancer and in the treatment of various other cancers and skin disorders.

Paritaprevir (ABT450) is an inhibitor of non-structural protein 3/4A protease with EC50 values of 1 and 0.21 nM for HCV 1a and HCV 1b, respectively.

1. Humantenmine is a toxic compound isolated from Gelsemium elegans Benth . 2. Humantenmine and koumine may inhibit several CYP450 enzyme activities.

Curcumenol ((+)-Curcumenol), one of the major components of Zedoary turmeric oil, is an antibiotic drug which has anti-Y, anti-inflammation activity. Curcumenol may be safely used without inducing metabolic drug-drug interaction through P450 inhibition.

(E)-Flavokawain A, a novel chalcone from kava extract, induces apoptosis in bladder cancer cells by involvement of Bax protein-dependent and mitochondria-dependent apoptotic pathway and suppresses tumor growth in mice.

CYP4A11/CYP4F2-IN-2 is a potent and orally active dual inhibitor of cytochrome P450 (CYP) 4A11 and CYP4F2, with IC50 values of 140 nM and 40 nM, respectively. Extractable from liver and kidney, CYP4A11/CYP4F2-IN-2 has the potential to treat kidney diseases.

Furafylline is a selective inhibitor of human cytochrome P450 (CYP)1A2 (IC50 : 0.07 µM),

N-Acetyl-L-aspartic acid is a derivative of aspartic acid, synthesized in neurons from the amino acid aspartic acid and acetyl coenzyme A. N-Acetyl-L-aspartic acid has antioxidant activity.

N-desmethyl Olanzapine is a metabolite of the atypical antipsychotic compound Olanzapinec, which is formed through the oxidative metabolism of olanzapine by the cytochrome 450 (CYP) isoenzyme CYP1A2.

5-Hydroxy-8-methoxypsoralen (5-Hydroxyxanthotoxin) is a potent tricyclic furocoumarin suicide inhibitor of CYP (cytochrome P-450) and a metabolite of Xanthotoxin. It is used in the treatment of psoriasis, eczema, vitiligo, and certain cutaneous lymphomas in combination with phototherapy involving exposure to sunlight.

Paritaprevir dihydrate (ABT-450), a highly effective and orally administered antiviral, acts as a non-structural protein 3/4A (NS3/4A) protease inhibitor, displaying EC50 values of 1 and 0.21 nM against HCV genotypes 1a and 1b, respectively. Additionally, it functions as a SARS-CoV 3CL pro inhibitor with an IC50 of 1.31 μM. Primarily metabolized by cytochrome P450 (CYP) 3A, its plasma concentration and half-life are significantly increased when administered with Ritonavir, a CYP450 inhibitor [1] [2] [3] [4].

4'-Methyl-β-naphthoflavone, a metabolite of naphthoflavones (benzoflavones) in fungi, acts as an activator or inhibitor of CYP-450 [1].