Drug Metabolite

Urolithin A is a secondary metabolite of ellagic acid, a polyphenolic antioxidant, that has antiproliferative, anti-inflammatory, and anti-oxidant properties.

Clozapine N-oxide is the major metabolite of Clozapine and is blood-brain barrier permeable. Clozapine N-oxide is an agonist of DREADDs and activates the DREADD receptors hM3Dq and hM4Di. Clozapine N-oxide is also a dopamine antagonist and selective muscarinic M4 receptor agonist.

Isonicotinic acid is a metabolite of Isoniazid.Isonicotinic acid is a useful isomer of nicotinic acid. Isoniazid is converted to Isonicotinic acid by hydrazinolysis, with the biotransformation also to be catalyzed by cytochrome P450 enzymes, such as CYP2C.

Mycophenolate Mofetil (TM-MMF), an immunosuppressive agent, is the 2-morpholinoethyl ester of mycophenolic acid (MPA), and an inhibitor of inosine monophosphate dehydrogenase (IMPDH).

Phosphoramide mustard is a toxic metabolite of cyclophosphamide with anticancer activity and ovarian toxicity that induces DNA damage.

6'-hydroxydihydrocinchonidine is a metabolite of quinine, with antimicrobial and antitumor activity, and inhibitory effect on Trypanosoma brucei and Streptococcus pneumoniae.

DL-Laudanosine (Laudanosine) is a recognized metabolite of atracurium and cisatracurium.

3-Sulfopropanoic acid, a major metabolite of treprostinil and its prodrug ALZ-801, is an endogenous molecule present in the cerebrospinal fluid (CSF) of AD patients that inhibits the formation of Aβ42 oligomers.

DP-1 hydrochloride is a degradation product of SDC-TRAP-0063, a fragment of Ganetespib, a heat shock protein 90 (HSP90) inhibitor with antitumor activity.

meta-Fexofenadine (meta-MDL-16455) is an isomer of Fexofenadine.

LGE-899 (Sonidegib metabolite M48) is a main metabolite of Sonidegib which is an inhibitor of the hedgehog pathway. The Tmax of LGE-899(60 h) is much longer than Sonidegib.

AST5902 mesylate is principal metabolite of Alflutinib in vivo. AST5902 mesylate exerts antineoplastic activity.

Didesethyl chloroquine (Bisdesethylchloroquine) is an effective myocardial inhibitor. Didesethyl chloroquine (Bisdesethylchloroquine) is the main metabolite of the antimalarial drug chloroquine.

2-Hydroxy atorvastatin calcium salt is a hydroxy metabolite of Atorvastatin calcium salt which is a potent HMG-CoA reductase inhibitor (IC50 = 8 nM).

4-Hydroxymephenytoin ((+/-)-4'-Hydroxymephenytoin) is the metabolism of an antiepileptic drug mephenytoin. Mephenytoin is used as a CYP2C19 substrate.

GS-829845 is a JAK1 inhibitor, the main component of the active metabolite of Filgotinib, which is approximately 10-fold less potent and has a longer half-life than the parent.

Methotrexate metabolite (DAMPA) (DAMPA) is the active metabolite of Methotrexate. Methotrexate is a folic acid antagonist. Methotrexate is used as a chemotherapeutic agent and immunosuppressant.

Allopurinol riboside is a metabolite of allopurinol with potency against parasites. Allopurinol riboside competitively inhibits the action of purine nucleoside phosphorylase on inosine with a Ki of 277 μM.

IMR-1A is the metabolite of IMR-1 which is a novel class of Notch inhibitors targeting the transcriptional activation with IC50 of 6 μMol/L.

Oseltamivir acid (GS4071) is a potent influenza virus neuraminidase inhibitor and the prodrug of GS4071.

(E/Z)-Endoxifen ((E/Z)-Endoxifen) is an active metabolite of tamoxifen produced by the sequential action of cytochrome P450 (CYP) isoforms, including CYP2D6. It is a strong anti-estrogen, as it has an approximately 100-fold greater affinity for estrogen receptors than tamoxifen. As the efficient conversion of tamoxifen to endoxifen depends on CYP2D6, polymorphisms in this CYP isoform can impact the effectiveness of TMX treatment.

Nortriptyline hydrochloride (ELF-101 hydrochloride) is a metabolite of AMITRIPTYLINE that is also used as an antidepressive agent. Nortriptyline is used in major depression, dysthymia, and atypical depressions.

Clofibric acid (Chlorofibrinic acid) is an antilipemic agent that is the biologically active metabolite of CLOFIBRATE.

Gentisuric acid, an Aspirin metabolite and a substrate of α-amidating monooxygenase (PAM), mitigates DNA damage induced by Mitomycin C. [1] [2]

4-Desmethoxy Omeprazole is the active metabolite of Omeprazole. Omeprazole is a proton pump inhibitor (PPI). Omeprazole shows competitive inhibition of CYP2C19 activity (Ki: 2 to 6 μM).

3-Hydroxycarbofuran, a principal metabolite of Carbofuran, acts as a reversible inhibitor of acetylcholinesterase (AChE) [1].

p,p'-DDE (p,p'-dichlorodiphenyldichloroethylene) is a metabolite and degradation product of the organochlorine pesticide DDT

Mebeverine acid (Mebeverine metabolite Mebeverine acid) is a secondary metabolite of Mebeverine and can be used as a marker of oral exposure to Mebeverine.

Quercetin 7-glucuronide (Quercetin 7-O-β-glucuronide), a Quercetin metabolite found in Madagascarian Uncarina species, has the capability to inhibit LDL oxidation [1].

16α-Hydroxyprednisolone is a stereoselective metabolite of the 22(R) epimer of the glucocorticoid budesonide

Compound 5, DDC 3′-O-β-D-glucuronide, is a drug metabolite with properties that inhibit the fibrillization and oligomerization of Aβ42, suggesting its potential utility in Alzheimer's disease research [1].

Leukotriene D4 (LTD4) is a potent pro-inflammatory mediator formed from arachidonic acid, a bronchoconstrictor, and induces osteoclast senescence.Leukotriene D4 induces transcriptional activity of potentially oncogenic genes and can be used in the study of asthma.

DCBA, an endogenous metabolite of the insect repellent N-N-diethyl-meta-toluamide (DEET), is utilized to evaluate DEET exposure through its concentration levels in urine.

Ampyrone (4-Aminoantipyrine) is a reagent for glucose determination in the presence of peroxidase and phenol.

N-(3-Methoxybenzyl-(9z,12z)-octadecadienamide ((9Z,12Z)-N-(3-Methoxybenzyl)octadeca-9,12-dienamide) is a Macamide impurity that may be used in the study of metabolic diseases.

Hydroxyhexamide ((±)-Hydroxyhexamid) is a pharmacologically active metabolite of Acetohexamide, used as a hypoglycemic agent.

N-Desmethylclozapine (Desmethylclozapine) is an antagonist of serotonin (5-HT) receptor subtype 5-HT2C (IC50: 7.1 nM). It also is an antagonist at dopamine D4 receptors, an agonist at δ-opioid receptors.

p-Coumaric Acid Ethyl Ester (Ethyl (E)-p-hydroxycinnamate) is the ethyl ester of p-Coumaric acid. p-Coumaric Acid is a common dietary polyphenol and also a potent immunosuppressive agent in treating autoimmune inflammatory diseases like rheumatoid arthritis.

Deslanoside (Desacetyllanatoside C) is a rapidly acting cardiac glycoside used to treat congestive heart failure and supraventricular arrhythmias due to reentry mechanisms. Deslanoside inhibits the Na-K-ATPase membrane pump, resulting in an increase in intracellular sodium and calcium concentrations.

Vinburnine (Eburnalritardo) is a vasodilator. Vinburnine is a vinca alkaloid and a metabolite of vincamine.

Omeprazole sulfide (Ufiprazole), a metabolite of Omeprazole, functions as a proton pump inhibitor.

Perindopril acyl-β-D-glucuronide is a metabolite of the ACE inhibitor perindopril [1].

RPR132595A (NPC) hydrochloride, an active metabolite of CPT-11, is produced via cytochrome P-450 3A4 (CYP3A4) metabolism and is ultimately eliminated via urinary excretion [1].

N-Desmethyl imatinib (Imatinib metabolite N-Desmethyl imatinib) is a metabolite of Imatinib, which is a multi-target inhibitor of c-Kit, v-Abl, and PDGFR.

GS-441524 was shown to be a safe and effective treatment for feline infectious peritonitis (FIP). The optimum dosage was found to be 4.0 mg/kg SC q24h for at least 12 weeks

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.

Dimetridazole is a nitroimidazole-based compound with antibacterial and anticoccidial activity. It was once widely used in the treatment of parasitic infections in poultry, cattle, swine and farmed fish until suspected to be carcinogenic and mutagenic to humans. Hydroxy dimetridazole is a metabolite of dimetridazole that may be useful for identifying this nitroimidazole in various agricultural samples through liquid chromatography-tandem mass spectrometry and other methods.

N-Acetylprocainamide (NAPA), the N-acetylated metabolite of Procainamide, is a Class III antiarrhythmic agent, while procainamide is a Class Ia antiarrhythmic drug.

Cycloguanil hydrochloride (Chloroguanide Triazine) is an active metabolite of the antimalarial compound proguanil. It acts as an inhibitor of dihydrofolate reductase (Kis: 0.3 and 1.5 nM for Plasmodium and human forms, respectively).

Norverapamil hydrochloride (D591 hydrochloride) ((±)-Norverapamil hydrochloride) is an N-demethylated metabolite of Verapamil and it is an L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.