Identification
- Summary
Letermovir is an antiviral medication used to treat CMV infections and disease in adult CMV-seropositive recipients of an allogeneic hematopoietic stem cell transplant (HSCT).
- Brand Names
- Prevymis
- Generic Name
- Letermovir
- DrugBank Accession Number
- DB12070
- Background
Letermovir recieved approval from the FDA on November 8th, 2017 for use in prophylaxis of cytomegalovirus (CMV) infection in allogeneic hematopoietic stem cell transplant patients 6. It represents the first entry into a new class of CMV anti-infectives, DNA terminase complex inhibitors 3. Letermovir has recieved both priority and orphan drug status from the FDA. It is currently marketed under the brand name Prevymis 6.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Letermovir (DB12070)
- Weight
- Average: 572.561
Monoisotopic: 572.20466805 - Chemical Formula
- C29H28F4N4O4
- Synonyms
- Letermovir
- External IDs
- AIC 246
- AIC-246
- AIC246
- MK-8228
Pharmacology
- Indication
For use in prophylaxis of cytomegalovirus (CMV) infection and disease in adult CMV-seropositive recipients of an allogeneic hematopoietic stem cell transplant (HSCT) Label.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- Pharmacodynamics
Letermovir inhibits the activity of the DNA terminase complex of CMV thereby preventing the cutting of viral DNA into mature length genomes for packaging into viral particles Label. Letemovir inhibits the DNA terminase complex with an EC50 of 2.1nM.
- Mechanism of action
CMV relies on a DNA terminase complex consisting of multiple subunits (pUL51, pUL56, and pUL89) for processing of viral DNA. Viral DNA is produced in a single repeating strand which is then cut by the DNA terminase complex into individual viral genomes which can then be packaged into mature viral particles 2. Letemovir inhibits the activity of this complex to prevent production of mature viral genomes and the production of viable viral particles. The exact nature of Letemovir's binding to this complex is not currently known. Initially, the observation of resistance-causing mutations in pUL56 suggested this subunit was the location of Letemovir binding 3. However, resistance mutations have now been observed in pUL51, pUL56, and pUL89 4. It is possible that changes in amino acid sequence in one subunit could result in conformational changes to interacting subunits affecting Letemovir binding or that Letemovir interacts with multiple subunits of the complex but evidence towards either of these distinctions has not yet been seen. pUL89 is known to contain the endonuclease activity of the complex but because all members of the complex are necessary for targeting as well as protection from proteosomal degradation, it is difficult to discern if Letemovir inhibits pUL89's activity directly 5.
Target Actions Organism ATripartite terminase subunit 1 inhibitorHuman Cytomegalovirus ATripartite terminase subunit 2 inhibitorHuman Cytomegalovirus ATripartite terminase subunit 3 inhibitorHuman Cytomegalovirus - Absorption
Letermovir has a bioavailability of 94% in healthy subjects when administered without cyclosporin, 35% in HSCT recipients when administered without cyclosporin, and 85% in HSCT recipients when administered with cyclosporin Label.
Letermovir's Tmax is 45 min to 2.25 h Label. Time to steady state has been observed to be 9-10 days.
Taking Letermovir with food increases Cmax by an average of 129.82% (range of 104.35%-161.50%) Label. No significant effect on AUC has been observed .
- Volume of distribution
The mean steady state volume of distrubution is 45.5L Label
- Protein binding
Letermovir has been observed to be 99% bound to plasma proteins at concentrations of 0.2-50 mg/L in vitro Label.
- Metabolism
Letermovir undergoes a minor degree of metabolism through UGT1A1/1A3 Label.
Hover over products below to view reaction partners
- Route of elimination
Letemovir is taken up by the liver through OATP1B1/3 transporters. 93% is excreted in the feces with 70% as the parent drug Label. <2% is excreted in the urine.
- Half-life
The mean terminal half-life was observed to be 12 hours following administration of Letemovir 480 mg IV once daily Label.
- Clearance
The mean clearance is 11.25 L/h in healthy subjects 1
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
There is no human data on the safety of Letemovir in pregnancy Label. Embryo-fetal toxicity and malformations have been observed in rats at exposures 11 times the human exposure at the recommended human dose (RHD) of Letemovir. No such toxicity was noted in rats at 3 times human exposure at the RHD or in rabbits at values less than human exposure with the RHD. Total litter loss was observed in 21.7% of female rats at 2 times human exposure at RHD. This did not occur at values similar to human exposure at RHD.
No human data is available regarding lactation Label. Letemovir has been observed in the milk of lactating rats and in the blood of their nursing pups.
No data is available concerning the effect of Letemovir on human fertility Label. Testicular toxicity leading to reduced fertility has been observed in male rats.
No antidote exists for Letemovir overdosage Label. The effectiveness of dialysis in clearing plasma of Letemovir is unknown.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- 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 softwareAbatacept The metabolism of Letermovir can be increased when combined with Abatacept. Abemaciclib The metabolism of Abemaciclib can be decreased when combined with Letermovir. Abiraterone The metabolism of Letermovir can be decreased when combined with Abiraterone. Abrocitinib The metabolism of Abrocitinib can be increased when combined with Letermovir. Acalabrutinib The metabolism of Acalabrutinib can be decreased when combined with Letermovir. Acamprosate The excretion of Acamprosate can be decreased when combined with Letermovir. Acebutolol The metabolism of Letermovir can be decreased when combined with Acebutolol. Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Letermovir. Acetaminophen The metabolism of Letermovir can be decreased when combined with Acetaminophen. Acetylcysteine The excretion of Letermovir can be decreased when combined with Acetylcysteine. 
Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more - Food Interactions
- Avoid St. John's Wort. Co-administration may lead to decreased serum concentrations of letermovir.
- Take with or without 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.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Prevymis Tablet, film coated 240 mg/1 Oral Merck Sharp & Dohme Llc 2017-11-08 Not applicable US 
Prevymis Injection, solution, concentrate 480 mg Intravenous Merck Sharp & Dohme B.V. 2021-02-10 Not applicable EU 
Prevymis Injection, solution 20 mg/1mL Intravenous Merck Sharp & Dohme Llc 2017-11-08 Not applicable US Prevymis Tablet, film coated 240 mg Oral Merck Sharp & Dohme B.V. 2021-02-10 Not applicable EU Prevymis Tablet 240 mg Oral Merck Ltd. 2017-12-20 Not applicable Canada 
Prevymis Injection, solution, concentrate 240 mg Intravenous Merck Sharp & Dohme B.V. 2021-02-10 Not applicable EU Prevymis Solution 20 mg / mL Intravenous Merck Ltd. 2017-12-20 Not applicable Canada Prevymis Tablet, film coated 480 mg/1 Oral Merck Sharp & Dohme Llc 2017-11-08 Not applicable US Prevymis Solution 20 mg / mL Intravenous Merck Ltd. 2017-12-20 Not applicable Canada Prevymis Tablet, film coated 480 mg Oral Merck Sharp & Dohme B.V. 2021-02-10 Not applicable EU
Categories
- ATC Codes
- J05AX18 — Letermovir
- Drug Categories
- Acids, Acyclic
- Anti-Infective Agents
- Antiinfectives for Systemic Use
- Antiviral Agents
- Antivirals for Systemic Use
- BCRP/ABCG2 Inhibitors
- BSEP/ABCB11 Inhibitors
- Cytochrome P-450 CYP2B6 Inducers
- Cytochrome P-450 CYP2B6 Inducers (strength unknown)
- Cytochrome P-450 CYP2C19 Inducers
- Cytochrome P-450 CYP2C19 Inducers (moderate)
- Cytochrome P-450 CYP2C8 Inhibitors
- Cytochrome P-450 CYP2C8 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2C9 Inducers
- Cytochrome P-450 CYP2C9 Inducers (strength unknown)
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A5 Inhibitors
- Cytochrome P-450 CYP3A5 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A7 Inhibitors
- Cytochrome P-450 CYP3A7 Inhibitors (strength unknown)
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Cytomegalovirus DNA Terminase Complex Inhibitor
- Direct Acting Antivirals
- DNA Terminase Complex Inhibitors
- Enzyme Inhibitors
- Fatty Acids
- Fatty Acids, Volatile
- Heterocyclic Compounds, Fused-Ring
- Lipids
- OAT3/SLC22A8 Inhibitors
- OATP1B1/SLCO1B1 Substrates
- OATP1B3 substrates
- Organic Anion Transporting Polypeptide 1B1 Inhibitors
- Organic Anion Transporting Polypeptide 1B3 Inhibitors
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- Poly(ADP-ribose) Polymerase Inhibitors
- UGT1A1 Substrates
- UGT1A3 substrates
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as phenylpiperazines. These are compounds containing a phenylpiperazine skeleton, which consists of a piperazine bound to a phenyl group.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Diazinanes
- Sub Class
- Piperazines
- Direct Parent
- Phenylpiperazines
- Alternative Parents
- N-arylpiperazines / Quinazolinamines / Trifluoromethylbenzenes / Aminophenyl ethers / Methoxyanilines / Anisoles / Dialkylarylamines / Phenoxy compounds / Methoxybenzenes / Alkyl aryl ethers show 12 more
- Substituents
- Alkyl aryl ether / Alkyl fluoride / Alkyl halide / Amine / Amino acid / Amino acid or derivatives / Aminophenyl ether / Aniline or substituted anilines / Anisole / Aromatic heteropolycyclic compound show 33 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Human Cytomegalovirus
Chemical Identifiers
- UNII
- 1H09Y5WO1F
- CAS number
- 917389-32-3
- InChI Key
- FWYSMLBETOMXAG-QHCPKHFHSA-N
- InChI
- InChI=1S/C29H28F4N4O4/c1-40-20-6-3-5-19(16-20)35-11-13-36(14-12-35)28-34-27-21(7-4-8-22(27)30)23(17-26(38)39)37(28)24-15-18(29(31,32)33)9-10-25(24)41-2/h3-10,15-16,23H,11-14,17H2,1-2H3,(H,38,39)/t23-/m0/s1
- IUPAC Name
- 2-[(4S)-8-fluoro-3-[2-methoxy-5-(trifluoromethyl)phenyl]-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3,4-dihydroquinazolin-4-yl]acetic acid
- SMILES
- COC1=CC=CC(=C1)N1CCN(CC1)C1=NC2=C(C=CC=C2F)[C@H](CC(O)=O)N1C1=CC(=CC=C1OC)C(F)(F)F
References
- Synthesis Reference
Humphrey GR, Dalby SM, Andreani T, Xiang B, Luzung MR, Song ZJ, Shevlin M, Christensen M, Belyk KM, Tschaen DM. 2016.Asymmetric Synthesis of Letermovir Using a Novel Phase-Transfer Catalyzed Aza-Michael Reaction. Org. Process Res. Dev. 20(6), 1097-1103. DOI: 10.1021/acs.oprd.6b00076
- General References
- Kropeit D, Scheuenpflug J, Erb-Zohar K, Halabi A, Stobernack HP, Hulskotte EGJ, van Schanke A, Zimmermann H, Rubsamen-Schaeff H: Pharmacokinetics and safety of letermovir, a novel anti-human cytomegalovirus drug, in patients with renal impairment. Br J Clin Pharmacol. 2017 Sep;83(9):1944-1953. doi: 10.1111/bcp.13292. Epub 2017 May 5. [Article]
- Goldner T, Hewlett G, Ettischer N, Ruebsamen-Schaeff H, Zimmermann H, Lischka P: The novel anticytomegalovirus compound AIC246 (Letermovir) inhibits human cytomegalovirus replication through a specific antiviral mechanism that involves the viral terminase. J Virol. 2011 Oct;85(20):10884-93. doi: 10.1128/JVI.05265-11. Epub 2011 Jul 13. [Article]
- Melendez DP, Razonable RR: Letermovir and inhibitors of the terminase complex: a promising new class of investigational antiviral drugs against human cytomegalovirus. Infect Drug Resist. 2015 Aug 5;8:269-77. doi: 10.2147/IDR.S79131. eCollection 2015. [Article]
- Chou S: A third component of the human cytomegalovirus terminase complex is involved in letermovir resistance. Antiviral Res. 2017 Dec;148:1-4. doi: 10.1016/j.antiviral.2017.10.019. Epub 2017 Oct 28. [Article]
- Neuber S, Wagner K, Goldner T, Lischka P, Steinbrueck L, Messerle M, Borst EM: Mutual Interplay between the Human Cytomegalovirus Terminase Subunits pUL51, pUL56, and pUL89 Promotes Terminase Complex Formation. J Virol. 2017 May 26;91(12). pii: e02384-16. doi: 10.1128/JVI.02384-16. Print 2017 Jun 15. [Article]
- FDA Approved Drugs: Letermovir [Link]
- External Links
- ChemSpider
- 26352849
- 1988648
- ChEMBL
- CHEMBL1241951
- ZINC
- ZINC000100369359
- Wikipedia
- Letermovir
- FDA label
- Download (1.86 MB)
- MSDS
- Download (22.3 KB)
Clinical Trials
- Clinical Trials
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, solution Intravenous 20 mg/1mL Injection, solution, concentrate Intravenous 240 MG Injection, solution, concentrate Intravenous 480 MG Solution Intravenous 20 mg / mL Tablet Oral 240 mg Tablet Oral 480 mg Tablet, film coated Oral 240 mg/1 Tablet, film coated Oral 480 mg/1 Tablet, film coated Oral 240 mg Solution Intravenous 240 mg Tablet, film coated Oral Injection, solution, concentrate Intravenous Tablet, film coated Oral 480 mg Tablet Oral Solution Intravenous 20 mg/ml Tablet, film coated Oral 240.0 mg Tablet, film coated Oral 480.0 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US7196086 No 2007-03-27 2024-05-22 US US8513255 No 2013-08-20 2024-05-22 US US10603384 No 2020-03-31 2033-02-28 US USRE46791 No 2018-04-17 2024-05-22 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.01 mg/mL ALOGPS logP 4.58 ALOGPS logP 4.64 Chemaxon logS -4.8 ALOGPS pKa (Strongest Acidic) 3.75 Chemaxon pKa (Strongest Basic) 7.15 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 8 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 77.84 Å2 Chemaxon Rotatable Bond Count 7 Chemaxon Refractivity 147.44 m3·mol-1 Chemaxon Polarizability 55 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Targets
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
- Kind
- Protein
- Organism
- Human Cytomegalovirus
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Component of the molecular motor that translocates viral genomic DNA in empty capsid during DNA packaging. Forms a tripartite terminase complex together with TRM2 and TRM3 in the host cytoplasm. Once the complex reaches the host nucleus, it interacts with the capsid portal vertex. This portal forms a ring in which genomic DNA is translocated into the capsid. TRM1 carries an endonuclease activity that plays an important role for the cleavage of concatemeric viral DNA into unit length genomes.
- Specific Function
- Atp binding
- Gene Name
- TRM1
- Uniprot ID
- F5HC79
- Uniprot Name
- Tripartite terminase subunit 1
- Molecular Weight
- 95810.305 Da
- Kind
- Protein
- Organism
- Human Cytomegalovirus
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Component of the molecular motor that translocates viral genomic DNA in empty capsid during DNA packaging. Forms a tripartite terminase complex together with TRM1 and TRM3 in the host cytoplasm. Once the complex reaches the host nucleus, it interacts with the capsid portal vertex. This portal forms a ring in which genomic DNA is translocated into the capsid.
- Specific Function
- Not Available
- Gene Name
- TRM2
- Uniprot ID
- F5HGI9
- Uniprot Name
- Tripartite terminase subunit 2
- Molecular Weight
- 16977.55 Da
- Kind
- Protein
- Organism
- Human Cytomegalovirus
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Component of the molecular motor that translocates viral genomic DNA in empty capsid during DNA packaging. Forms a tripartite terminase complex together with TRM1 and TRM2 in the host cytoplasm. Once the complex reaches the host nucleus, it interacts with the capsid portal vertex. This portal forms a ring in which genomic DNA is translocated into the capsid. TRM3 carries an RNase H-like nuclease activity that plays an important role for the cleavage of concatemeric viral DNA into unit length genomes.
- Specific Function
- Dna binding
- Gene Name
- TRM3
- Uniprot ID
- F5HCU8
- Uniprot Name
- Tripartite terminase subunit 3
- Molecular Weight
- 77033.575 Da
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Steroid binding
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
- Gene Name
- UGT1A1
- Uniprot ID
- P22309
- Uniprot Name
- UDP-glucuronosyltransferase 1-1
- Molecular Weight
- 59590.91 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Retinoic acid binding
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. Isoform 2 lacks transferase activity but acts as a negative reg...
- Gene Name
- UGT1A3
- Uniprot ID
- P35503
- Uniprot Name
- UDP-glucuronosyltransferase 1-3
- Molecular Weight
- 60337.835 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- 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
- CYP2C8
- Uniprot ID
- P10632
- Uniprot Name
- Cytochrome P450 2C8
- Molecular Weight
- 55824.275 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inducer
- 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
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inducer
- 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
- Marshall WL, McCrea JB, Macha S, Menzel K, Liu F, van Schanke A, de Haes JIU, Hussaini A, Jordan HR, Drexel M, Kantesaria BS, Tsai C, Cho CR, Hulskotte EGJ, Butterton JR, Iwamoto M: Pharmacokinetics and Tolerability of Letermovir Coadministered With Azole Antifungals (Posaconazole or Voriconazole) in Healthy Subjects. J Clin Pharmacol. 2018 Jul;58(7):897-904. doi: 10.1002/jcph.1094. Epub 2018 Mar 26. [Article]
- Letermovir FDA label [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inducer
- 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
- CYP2B6
- Uniprot ID
- P20813
- Uniprot Name
- Cytochrome P450 2B6
- Molecular Weight
- 56277.81 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- 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
- FDA Approved Drugs: Letermovir [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Oxygen binding
- 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
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Oxygen binding
- 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
- CYP3A7
- Uniprot ID
- P24462
- Uniprot Name
- Cytochrome P450 3A7
- Molecular Weight
- 57525.03 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Monooxygenase activity
- Specific Function
- Exhibits low testosterone 6-beta-hydroxylase activity.
- Gene Name
- CYP3A43
- Uniprot ID
- Q9HB55
- Uniprot Name
- Cytochrome P450 3A43
- Molecular Weight
- 57669.21 Da
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
- Gene Name
- SLCO1B1
- Uniprot ID
- Q9Y6L6
- Uniprot Name
- Solute carrier organic anion transporter family member 1B1
- Molecular Weight
- 76447.99 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
- Gene Name
- SLCO1B3
- Uniprot ID
- Q9NPD5
- Uniprot Name
- Solute carrier organic anion transporter family member 1B3
- Molecular Weight
- 77402.175 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
- Gene Name
- ABCG2
- Uniprot ID
- Q9UNQ0
- Uniprot Name
- ATP-binding cassette sub-family G member 2
- Molecular Weight
- 72313.47 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Transporter activity
- Specific Function
- Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
- Gene Name
- ABCB11
- Uniprot ID
- O95342
- Uniprot Name
- Bile salt export pump
- Molecular Weight
- 146405.83 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
- Gene Name
- SLC22A8
- Uniprot ID
- Q8TCC7
- Uniprot Name
- Solute carrier family 22 member 8
- Molecular Weight
- 59855.585 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Organic anion transmembrane transporter activity
- Specific Function
- Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
- Gene Name
- ABCC2
- Uniprot ID
- Q92887
- Uniprot Name
- Canalicular multispecific organic anion transporter 1
- Molecular Weight
- 174205.64 Da
Drug created at October 20, 2016 21:18 / Updated at March 21, 2023 17:58