Identification
- Summary
Aprepitant is a substance P/neurokinin 1 receptor antagonist used to treat nausea and vomiting caused by chemotherapy and surgery.
- Brand Names
- Aponvie, Cinvanti, Emend
- Generic Name
- Aprepitant
- DrugBank Accession Number
- DB00673
- Background
Aprepitant, an antiemetic, is a substance P/neurokinin 1 (NK1) receptor antagonist which, in combination with other antiemetic agents, is indicated for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. Aprepitant has little or no affinity for serotonin (5-HT3), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting (CI NV).
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Aprepitant (DB00673)
- Weight
- Average: 534.4267
Monoisotopic: 534.150187993 - Chemical Formula
- C23H21F7N4O3
- Synonyms
- Aprepitant
- Aprépitant
- Aprepitantum
- External IDs
- L 754030
- L-754,030
- L-754939
- MK-0869
- MK-869
Pharmacology
- Indication
For the prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy, including high-dose cisplatin (in combination with other antiemetic agents).
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Adjunct therapy in prevention of Chemotherapy-induced nausea and vomiting (cinv) •••••••••••• ••••••• Adjunct therapy in prevention of Chemotherapy-induced nausea and vomiting (cinv) •••••••••••• •••••••••• •••••••••• Prevention of Chemotherapy-induced nausea and vomiting (cinv) •••••••••••• •••••••••• Prevention of Chemotherapy-induced nausea and vomiting (cinv) •••••••••••• ••••• Adjunct therapy in prevention of Chemotherapy-induced nausea and vomiting (cinv) •••••••••••• ••••• - Contraindications & Blackbox Warnings
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Aprepitant, an antiemetic, is a substance P/neurokinin 1 (NK1) receptor antagonist which, in combination with other antiemetic agents, is indicated for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. Aprepitant has little or no affinity for serotonin (5-HT3), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting (CI NV).
- Mechanism of action
Aprepitant has been shown in animal models to inhibit emesis induced by cytotoxic chemotherapeutic agents, such as cisplatin, via central actions. Animal and human Positron Emission Tomography (PET) studies with Aprepitant have shown that it crosses the blood brain barrier and occupies brain NK1 receptors. Animal and human studies show that Aprepitant augments the antiemetic activity of the 5-HT3-receptor antagonist ondansetron and the corticosteroid ethasone and inhibits both the acute and delayed phases of cisplatin induced emesis.
Target Actions Organism ANeurokinin 1 receptor antagonistHumans - Absorption
The mean absolute oral bioavailability of aprepitant is approximately 60 to 65%.
- Volume of distribution
- 70 L
- Protein binding
Protein binding is reported to be >95%.
- Metabolism
Aprepitant primarily undergoes CYP3A4-mediated metabolism, as well as minor metabolism mediated by CYP1A2 and CYP2C19. About seven metabolites of aprepitant have been identified in human plasma, which all retain weak pharmacological activity.
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- Route of elimination
Aprepitant is eliminated primarily by metabolism; aprepitant is not renally excreted. Aprepitant is excreted in the milk of rats. It is not known whether this drug is excreted in human milk.
- Half-life
9-13 hours
- Clearance
- Apparent plasma cl=62-90 mL/min
- Adverse Effects
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Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The metabolism of 1,2-Benzodiazepine can be decreased when combined with Aprepitant. Abametapir The serum concentration of Aprepitant can be increased when it is combined with Abametapir. Abatacept The metabolism of Aprepitant can be increased when combined with Abatacept. Abemaciclib The metabolism of Abemaciclib can be decreased when combined with Aprepitant. Abiraterone The metabolism of Abiraterone can be decreased when combined with Aprepitant. - Food Interactions
- Take with or without food. The absorption is unaffected by food.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Images
- International/Other Brands
- Aprecap (Glenmark)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Aponvie Emulsion 32 mg/4.4mL Intravenous Heron Therapeutics, Inc. 2023-03-06 Not applicable US 
Cinvanti Injection, emulsion 130 mg/18mL Intravenous Heron Therapeutics, Inc. 2018-01-03 Not applicable US Emend Capsule 40 mg Oral Merck Sharp & Dohme B.V. 2016-09-08 Not applicable EU 
Emend Capsule 80 mg Oral Merck Sharp & Dohme B.V. 2016-09-08 Not applicable EU Emend Powder, for suspension 125 mg/1 Oral Merck Sharp & Dohme Llc 2015-12-17 Not applicable US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Aprepitant Capsule 40 mg/1 Oral Torrent Pharmaceuticals Limited 2020-10-21 Not applicable US Aprepitant Capsule 40 mg/1 Oral Glenmark Pharmaceuticals Inc., USA 2017-10-12 Not applicable US Aprepitant Capsule 40 mg/1 Oral Sandoz Inc 2016-12-27 Not applicable US Aprepitant Capsule 125 mg/1 Oral Torrent Pharmaceuticals Limited 2020-10-21 Not applicable US Aprepitant Capsule 125 mg/1 Oral Glenmark Pharmaceuticals Inc., USA 2017-10-12 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Aprepitant Aprepitant (80 mg/1) + Aprepitant (125 mg/1) Capsule; Kit Oral Torrent Pharmaceuticals Limited 2020-10-21 Not applicable US Aprepitant Aprepitant (80 mg/1) + Aprepitant (125 mg/1) Capsule; Kit Oral Glenmark Pharmaceuticals Inc., USA 2017-10-12 Not applicable US Aprepitant Aprepitant (80 mg/1) + Aprepitant (125 mg/1) Capsule; Kit Oral Sandoz Inc 2016-12-27 Not applicable US Aprepitant Aprepitant (80 mg/1) + Aprepitant (125 mg/1) Capsule; Kit Oral Torrent Pharmaceuticals Limited 2020-10-21 Not applicable US Aprepitant Aprepitant (80 mg/1) + Aprepitant (125 mg/1) Capsule; Kit Oral Sandoz Inc 2016-12-27 Not applicable US
Categories
- ATC Codes
- A04AD12 — Aprepitant
- Drug Categories
- Alimentary Tract and Metabolism
- Antiemetics
- Antiemetics and Antinauseants
- Aprepitant and Prodrugs
- Autonomic Agents
- Central Nervous System Agents
- Cytochrome P-450 CYP2C19 Inhibitors
- Cytochrome P-450 CYP2C19 Inhibitors (weak)
- Cytochrome P-450 CYP2C19 Substrates
- Cytochrome P-450 CYP2C9 Inducers
- Cytochrome P-450 CYP2C9 Inducers (strength unknown)
- Cytochrome P-450 CYP2C9 Inhibitors
- Cytochrome P-450 CYP2C9 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2C9 Inhibitors (weak)
- Cytochrome P-450 CYP3A Inducers
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inducers
- Cytochrome P-450 CYP3A4 Inducers (strength unknown)
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (moderate)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Inhibitors
- Cytochrome P-450 CYP3A5 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 CYP3A7 Inhibitors
- Cytochrome P-450 CYP3A7 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A7 Substrates
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Gastrointestinal Agents
- Morpholines
- Neurokinin 1 Antagonists
- Neurokinin-1 Receptor Antagonists
- Neurotransmitter Agents
- Oxazines
- Peripheral Nervous System Agents
- Substance P/Neurokinin-1 Receptor Antagonist
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as phenylmorpholines. These are aromatic compounds containing a morpholine ring and a benzene ring linked to each other through a CC or a CN bond.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Oxazinanes
- Sub Class
- Morpholines
- Direct Parent
- Phenylmorpholines
- Alternative Parents
- Trifluoromethylbenzenes / Fluorobenzenes / Aralkylamines / Aryl fluorides / Triazoles / Heteroaromatic compounds / Trialkylamines / Oxacyclic compounds / Azacyclic compounds / Acetals show 5 more
- Substituents
- 1,2,4-triazole / Acetal / Alkyl fluoride / Alkyl halide / Amine / Aralkylamine / Aromatic heteromonocyclic compound / Aryl fluoride / Aryl halide / Azacycle show 20 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- morpholines, triazoles, (trifluoromethyl)benzenes, cyclic acetal (CHEBI:499361)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 1NF15YR6UY
- CAS number
- 170729-80-3
- InChI Key
- ATALOFNDEOCMKK-OITMNORJSA-N
- InChI
- InChI=1S/C23H21F7N4O3/c1-12(14-8-15(22(25,26)27)10-16(9-14)23(28,29)30)37-20-19(13-2-4-17(24)5-3-13)34(6-7-36-20)11-18-31-21(35)33-32-18/h2-5,8-10,12,19-20H,6-7,11H2,1H3,(H2,31,32,33,35)/t12-,19+,20-/m1/s1
- IUPAC Name
- 3-{[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl}-4,5-dihydro-1H-1,2,4-triazol-5-one
- SMILES
- C[C@@H](O[C@H]1OCCN(CC2=NNC(=O)N2)[C@H]1C1=CC=C(F)C=C1)C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F
References
- Synthesis Reference
Mangesh Shivram Sawant, Girish Dixit, Nitin Sharad Chandra Pradhan, Mubeen Ahmad Khan, Sukumar Sinha, "Amorphous and Crystalline Forms of Aprepitant and Processes for the Preparation Thereof." U.S. Patent US20090192161, issued July 30, 2009.
US20090192161- General References
- External Links
- Human Metabolome Database
- HMDB0014811
- KEGG Drug
- D02968
- PubChem Compound
- 6918365
- PubChem Substance
- 46505211
- ChemSpider
- 5293568
- BindingDB
- 50220136
- 358255
- ChEBI
- 499361
- ChEMBL
- CHEMBL1471
- ZINC
- ZINC000027428713
- Therapeutic Targets Database
- DNC000952
- PharmGKB
- PA164747039
- PDBe Ligand
- GBQ
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Aprepitant
- PDB Entries
- 6hlo / 6j20 / 6j21
- FDA label
- Download (293 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Active Not Recruiting Prevention Obesity / Post Operative Nausea and Vomiting (PONV) 1 4 Completed Not Available Healthy Subjects (HS) 1 4 Completed Prevention Breast Neoplasms / Nausea / Vomiting 1 4 Completed Prevention Chemotherapy-Induced Nausea and Vomiting 1 4 Completed Prevention Nausea / Post Operative Nausea and Vomiting (PONV) 1
Pharmacoeconomics
- Manufacturers
- Merck and co inc
- Packagers
- Merck & Co.
- Physicians Total Care Inc.
- Dosage Forms
Form Route Strength Emulsion Intravenous 32 mg/4.4mL Capsule Oral 125 MG/80MG Capsule Oral 125 mg/1 Capsule; kit Oral Powder Not applicable 1 kg/1kg Capsule Oral Capsule Oral Injection, emulsion Intravenous 130 mg/18mL Capsule Oral 125.000 mg Capsule Oral 165 mg Capsule Oral 40 mg Capsule Oral 40 mg/1 Capsule Oral 80 mg/1 Kit Oral Powder, for suspension Oral 125 mg/1 Powder, for suspension Oral 125 MG Capsule, coated Oral 165 mg Capsule, coated Oral Powder, for solution Intravenous; Parenteral Capsule Oral 125.00 mg Capsule Oral 80.00 mg Powder, for solution Intravenous; Parenteral 115 MG Powder, for solution Intravenous; Parenteral 150 MG Capsule, coated Oral 40 mg Capsule Oral 80.000 mg Capsule Oral 125 mg Capsule Oral 80 mg - Prices
Unit description Cost Unit Emend 6 125 mg capsule Box 1046.01USD box Emend 6 80 mg capsule Box 678.62USD box Emend 5 80 mg capsule Box 553.13USD box Emend 3 80 & 125 mg capsule Disp Pack 415.76USD disp Emend 115 mg Solution 1 Vial = 10ml 242.13USD vial Emend 115 mg vial 232.82USD vial Emend 2 80 mg capsule Disp Pack 226.21USD disp Emend 125 mg capsule 161.34USD capsule Emend 80 mg capsule 108.76USD capsule Emend 40 mg capsule Box 58.17USD box Emend 40 mg capsule 55.89USD capsule DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5145684 No 1992-09-08 2011-01-25 US CA2469315 No 2008-12-02 2022-12-19 Canada 
US8258132 No 2012-09-04 2027-09-26 US US6096742 No 2000-08-01 2018-07-01 US US9561229 No 2017-02-07 2035-09-18 US US9808465 No 2017-11-07 2035-09-18 US US9974794 No 2018-05-22 2035-09-18 US US9974793 No 2018-05-22 2035-09-18 US US9974742 No 2018-05-22 2035-09-18 US US10500208 No 2019-12-10 2035-09-18 US US10624850 No 2020-04-21 2035-09-18 US US10953018 No 2021-03-23 2035-09-18 US US11173118 No 2021-11-16 2035-09-18 US US11744800 No 2015-09-18 2035-09-18 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility Practically insoluble Not Available logP 4.5 Not Available - Predicted Properties
Property Value Source Water Solubility 0.0194 mg/mL ALOGPS logP 2.44 ALOGPS logP 5.22 Chemaxon logS -4.4 ALOGPS pKa (Strongest Acidic) 6.59 Chemaxon pKa (Strongest Basic) 3.63 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 75.19 Å2 Chemaxon Rotatable Bond Count 8 Chemaxon Refractivity 116.93 m3·mol-1 Chemaxon Polarizability 45.55 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 0 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9952 Blood Brain Barrier + 0.5588 Caco-2 permeable - 0.6237 P-glycoprotein substrate Substrate 0.8106 P-glycoprotein inhibitor I Inhibitor 0.5243 P-glycoprotein inhibitor II Non-inhibitor 0.9564 Renal organic cation transporter Non-inhibitor 0.7444 CYP450 2C9 substrate Non-substrate 0.788 CYP450 2D6 substrate Non-substrate 0.9115 CYP450 3A4 substrate Substrate 0.6461 CYP450 1A2 substrate Non-inhibitor 0.6012 CYP450 2C9 inhibitor Non-inhibitor 0.535 CYP450 2D6 inhibitor Non-inhibitor 0.84 CYP450 2C19 inhibitor Non-inhibitor 0.5862 CYP450 3A4 inhibitor Inhibitor 0.5 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.8396 Ames test Non AMES toxic 0.5758 Carcinogenicity Non-carcinogens 0.8152 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 2.6055 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.6598 hERG inhibition (predictor II) Inhibitor 0.8163
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 204.309183 predictedDarkChem Lite v0.1.0 [M-H]- 208.83667 predictedDeepCCS 1.0 (2019) [M+H]+ 204.010983 predictedDarkChem Lite v0.1.0 [M+H]+ 211.23224 predictedDeepCCS 1.0 (2019) [M+Na]+ 204.093183 predictedDarkChem Lite v0.1.0 [M+Na]+ 217.1054 predictedDeepCCS 1.0 (2019)
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Tachykinin receptor activity
- Specific Function
- This is a receptor for the tachykinin neuropeptide substance P. It is probably associated with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of aff...
- Gene Name
- TACR1
- Uniprot ID
- P25103
- Uniprot Name
- Substance-P receptor
- Molecular Weight
- 46250.5 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Brands KM, Payack JF, Rosen JD, Nelson TD, Candelario A, Huffman MA, Zhao MM, Li J, Craig B, Song ZJ, Tschaen DM, Hansen K, Devine PN, Pye PJ, Rossen K, Dormer PG, Reamer RA, Welch CJ, Mathre DJ, Tsou NN, McNamara JM, Reider PJ: Efficient synthesis of NK(1) receptor antagonist aprepitant using a crystallization-induced diastereoselective transformation. J Am Chem Soc. 2003 Feb 26;125(8):2129-35. [Article]
- Rodgers J, Bradley B, Kennedy PG: Combination chemotherapy with a substance P receptor antagonist (aprepitant) and melarsoprol in a mouse model of human African trypanosomiasis. Parasitol Int. 2007 Dec;56(4):321-4. Epub 2007 Jun 29. [Article]
- Poli-Bigelli S, Rodrigues-Pereira J, Carides AD, Julie Ma G, Eldridge K, Hipple A, Evans JK, Horgan KJ, Lawson F: Addition of the neurokinin 1 receptor antagonist aprepitant to standard antiemetic therapy improves control of chemotherapy-induced nausea and vomiting. Results from a randomized, double-blind, placebo-controlled trial in Latin America. Cancer. 2003 Jun 15;97(12):3090-8. [Article]
- Zhao MM, McNamara JM, Ho GJ, Emerson KM, Song ZJ, Tschaen DM, Brands KM, Dolling UH, Grabowski EJ, Reider PJ, Cottrell IF, Ashwood MS, Bishop BC: Practical asymmetric synthesis of aprepitant, a potent human NK-1 receptor antagonist, via a stereoselective Lewis acid-catalyzed trans acetalization reaction. J Org Chem. 2002 Sep 20;67(19):6743-7. [Article]
- Bergstrom M, Hargreaves RJ, Burns HD, Goldberg MR, Sciberras D, Reines SA, Petty KJ, Ogren M, Antoni G, Langstrom B, Eskola O, Scheinin M, Solin O, Majumdar AK, Constanzer ML, Battisti WP, Bradstreet TE, Gargano C, Hietala J: Human positron emission tomography studies of brain neurokinin 1 receptor occupancy by aprepitant. Biol Psychiatry. 2004 May 15;55(10):1007-12. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitorInducer
- Curator comments
- One study mentions that Aprepitant is a moderate inducer of CYP3A4.
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Sanchez RI, Wang RW, Newton DJ, Bakhtiar R, Lu P, Chiu SH, Evans DC, Huskey SE: Cytochrome P450 3A4 is the major enzyme involved in the metabolism of the substance P receptor antagonist aprepitant. Drug Metab Dispos. 2004 Nov;32(11):1287-92. Epub 2004 Aug 10. [Article]
- Majumdar AK, McCrea JB, Panebianco DL, Hesney M, Dru J, Constanzer M, Goldberg MR, Murphy G, Gottesdiener KM, Lines CR, Petty KJ, Blum RA: Effects of aprepitant on cytochrome P450 3A4 activity using midazolam as a probe. Clin Pharmacol Ther. 2003 Aug;74(2):150-6. doi: 10.1016/S0009-9236(03)00123-1. [Article]
- Dando TM, Perry CM: Aprepitant: a review of its use in the prevention of chemotherapy-induced nausea and vomiting. Drugs. 2004;64(7):777-94. [Article]
- Flockhart Table of Drug Interactions [Link]
- FDA Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- Molecular Weight
- 55930.545 Da
References
- Sanchez RI, Wang RW, Newton DJ, Bakhtiar R, Lu P, Chiu SH, Evans DC, Huskey SE: Cytochrome P450 3A4 is the major enzyme involved in the metabolism of the substance P receptor antagonist aprepitant. Drug Metab Dispos. 2004 Nov;32(11):1287-92. Epub 2004 Aug 10. [Article]
- House L, Ramirez J, Seminerio M, Mirkov S, Ratain MJ: In vitro glucuronidation of aprepitant: a moderate inhibitor of UGT2B7. Xenobiotica. 2015;45(11):990-8. doi: 10.3109/00498254.2015.1038743. Epub 2015 Jun 8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- InhibitorInducer
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- Dando TM, Perry CM: Aprepitant: a review of its use in the prevention of chemotherapy-induced nausea and vomiting. Drugs. 2004;64(7):777-94. [Article]
- Navari RM: Aprepitant: a neurokinin-1 receptor antagonist for the treatment of chemotherapy-induced nausea and vomiting. Expert Rev Anticancer Ther. 2004 Oct;4(5):715-24. doi: 10.1586/14737140.4.5.715. [Article]
- Sanchez RI, Wang RW, Newton DJ, Bakhtiar R, Lu P, Chiu SH, Evans DC, Huskey SE: Cytochrome P450 3A4 is the major enzyme involved in the metabolism of the substance P receptor antagonist aprepitant. Drug Metab Dispos. 2004 Nov;32(11):1287-92. Epub 2004 Aug 10. [Article]
- Aprepitant FDA label [File]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55