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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyIdentification
- Name
- Lopinavir
- Accession Number
- DB01601 (EXPT00388)
- Type
- Small Molecule
- Groups
- Approved
- Description
Lopinavir (ABT-378) is an antiretroviral of the protease inhibitor class. It is marketed by Abbott as Kaletra, a co-formulation with a sub-therapeutic dose of ritonavir, as a component of combination therapy to treat HIV/AIDS.
- Structure
Structure for Lopinavir (DB01601)
- Synonyms
- LPV
- External IDs
- A-157378-0 / A-157378.0 / ABT-378
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Kaletra Lopinavir (133.3 mg) + Ritonavir (33.3 mg) Capsule Oral Abbvie 2001-03-09 2012-11-02 Canada 
Kaletra Lopinavir (100 mg/1) + Ritonavir (25 mg/1) Tablet, film coated Oral Abbvie 2010-06-18 Not applicable US 
Kaletra Lopinavir (80 mg) + Ritonavir (20 mg) Solution Oral Abbvie 2001-03-09 Not applicable Canada Kaletra Lopinavir (200 mg/1) + Ritonavir (50 mg/1) Tablet, film coated Oral Remedy Repack 2008-09-05 2017-01-16 US Kaletra Lopinavir (200 mg/1) + Ritonavir (50 mg/1) Tablet, film coated Oral Dispensing Solutions, Inc. 2010-06-18 Not applicable US Kaletra Lopinavir (200 mg/1) + Ritonavir (50 mg/1) Tablet, film coated Oral Physicians Total Care, Inc. 2006-04-11 Not applicable US Kaletra Lopinavir (200 mg/1) + Ritonavir (50 mg/1) Tablet, film coated Oral Pd Rx Pharmaceuticals, Inc. 2010-06-18 Not applicable US Kaletra Lopinavir (200 mg/1) + Ritonavir (50 mg/1) Tablet, film coated Oral Abbvie 2010-06-18 Not applicable US Kaletra Lopinavir (100 mg) + Ritonavir (25 mg) Tablet Oral Abbvie 2008-08-11 Not applicable Canada Kaletra Lopinavir (200 mg/1) + Ritonavir (50 mg/1) Tablet, film coated Oral A-S Medication Solutions 2010-06-18 Not applicable US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Kaletra Lopinavir (200 mg/1) + Ritonavir (50 mg/1) Tablet Oral Remedy Repack 2010-09-27 2013-05-16 US - International/Other Brands
- Aluviran / Koletra
- Categories
- Anti-HIV Agents
- Anti-Infective Agents
- Anti-Retroviral Agents
- Antiinfectives for Systemic Use
- Antiviral Agents
- Antivirals for Systemic Use
- BSEP/ABCB11 Substrates
- Chemically-Induced Disorders
- CYP3A Substrates (Sensitive)
- Cytochrome P-450 CYP2B6 Inhibitors
- Cytochrome P-450 CYP2B6 Inhibitors (weak)
- Cytochrome P-450 CYP2C19 Inhibitors
- Cytochrome P-450 CYP2C19 Inhibitors (weak)
- Cytochrome P-450 CYP2C8 Inhibitors
- Cytochrome P-450 CYP2C8 Inhibitors (strong)
- Cytochrome P-450 CYP2C9 Inducers
- Cytochrome P-450 CYP2C9 Inhibitors
- Cytochrome P-450 CYP2C9 Inhibitors (weak)
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (moderate)
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Inhibitors (strong)
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (strong)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P450 3A Inhibitors
- Direct Acting Antivirals
- Enzyme Inhibitors
- Highest Risk QTc-Prolonging Agents
- HIV Protease Inhibitors
- Hyperglycemia-Associated Agents
- Nephrotoxic agents
- OATP1B1/SLCO1B1 Inhibitors
- OATP1B3 transporter inhibitors
- Organic Anion Transporting Polypeptide 1B1 Inhibitors
- P-glycoprotein/ABCB1 Inhibitors
- Protease Inhibitors
- Pyrimidines
- Pyrimidinones
- QTc Prolonging Agents
- UNII
- 2494G1JF75
- CAS number
- 192725-17-0
- Weight
- Average: 628.8008
Monoisotopic: 628.362470666 - Chemical Formula
- C37H48N4O5
- InChI Key
- KJHKTHWMRKYKJE-SUGCFTRWSA-N
- InChI
- InChI=1S/C37H48N4O5/c1-25(2)34(41-20-12-19-38-37(41)45)36(44)39-30(21-28-15-7-5-8-16-28)23-32(42)31(22-29-17-9-6-10-18-29)40-33(43)24-46-35-26(3)13-11-14-27(35)4/h5-11,13-18,25,30-32,34,42H,12,19-24H2,1-4H3,(H,38,45)(H,39,44)(H,40,43)/t30-,31-,32-,34-/m0/s1
- IUPAC Name
- (2S)-N-[(2S,4S,5S)-5-[2-(2,6-dimethylphenoxy)acetamido]-4-hydroxy-1,6-diphenylhexan-2-yl]-3-methyl-2-(2-oxo-1,3-diazinan-1-yl)butanamide
- SMILES
- CC(C)[C@H](N1CCCNC1=O)C(=O)N[C@H](C[C@H](O)[C@H](CC1=CC=CC=C1)NC(=O)COC1=C(C)C=CC=C1C)CC1=CC=CC=C1
Pharmacology
- Indication
Indicated in combination with other antiretroviral agents for the treatment of HIV-infection.
- Associated Conditions
- Pharmacodynamics
Lopinavir is an antiretroviral of the protease inhibitor class. Inhibiting HIV-1 protease (responsible for protein cleavage), results in selectively inhibiting the cleavage of HIV gag and gag-pol polyproteins, thereby preventing viral maturation.
- Mechanism of action
Lopinavir inhibits the HIV viral protease enzyme. This prevents cleavage of the gag-pol polyprotein and, therefore, improper viral assembly results. This subsequently results in non-infectious, immature viral particles.
Target Actions Organism AHuman immunodeficiency virus type 1 protease inhibitorHuman immunodeficiency virus 1 - Absorption
Administered alone, lopinavir has insufficient bioavailability; however, like several HIV protease inhibitors, its blood levels are greatly increased by low doses of ritonavir, a potent inhibitor of cytochrome P450 3A4.
- Volume of distribution
- Not Available
- Protein binding
Lopinavir is highly bound to plasma proteins (98-99%).
- Metabolism
Hepatic. Lopinavir is extensively metabolized by the hepatic cytochrome P450 system, almost exclusively by the CYP3A isozyme.
- Route of elimination
- Not Available
- Half life
- Not Available
- Clearance
- Not Available
- Toxicity
Although human experience of acute overdosage with lopinavir is limited, accidental ingestion of the product by a young child could result in significant alcohol-related toxicity and could approach the potential lethal dose of alcohol.
- Affected organisms
- Human Immunodeficiency Virus
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
Drug Interaction 16-Bromoepiandrosterone The serum concentration of 16-Bromoepiandrosterone can be increased when it is combined with Lopinavir. 19-norandrostenedione The serum concentration of 19-norandrostenedione can be increased when it is combined with Lopinavir. 2,4-thiazolidinedione The therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Lopinavir. 4-Methoxyamphetamine The metabolism of 4-Methoxyamphetamine can be decreased when combined with Lopinavir. 5-androstenedione The serum concentration of 5-androstenedione can be increased when it is combined with Lopinavir. Abemaciclib The risk or severity of adverse effects can be increased when Lopinavir is combined with Abemaciclib. Abiraterone The metabolism of Abiraterone can be decreased when combined with Lopinavir. ABT-341 The therapeutic efficacy of (1S,6R)-3-{[3-(TRIFLUOROMETHYL)-5,6-DIHYDRO[1,2,4]TRIAZOLO[4,3-A]PYRAZIN-7(8H)-YL]CARBONYL}-6-(2,4,5-TRIFLUOROPHENYL)CYCLOHEX-3-EN-1-AMINE can be decreased when used in combination with Lopinavir. Acarbose The therapeutic efficacy of Acarbose can be decreased when used in combination with Lopinavir. Acebutolol The serum concentration of Acebutolol can be increased when it is combined with Lopinavir. - Food Interactions
- Avoid St.John's Wort.
- Take with food.
References
- Synthesis Reference
- US5914332
- General References
- Not Available
- External Links
- Human Metabolome Database
- HMDB0015539
- KEGG Drug
- D01425
- KEGG Compound
- C12871
- PubChem Compound
- 92727
- PubChem Substance
- 46508588
- ChemSpider
- 83706
- BindingDB
- 578
- ChEBI
- 31781
- ChEMBL
- CHEMBL729
- Therapeutic Targets Database
- DAP000708
- PharmGKB
- PA450264
- HET
- AB1
- RxList
- RxList Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Lopinavir
- ATC Codes
- J05AR10 — Lopinavir and ritonavir
- PDB Entries
- 1mui / 1rv7 / 2o4s / 2q5k / 2qhc / 2rkf / 2rkg / 2z54 / 3ogq / 4l1a
Clinical Trials
- Clinical Trials
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage forms
Form Route Strength Capsule Oral Capsule, liquid filled Oral Solution Oral Tablet Oral Tablet, film coated Oral - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) US6703403 Yes 1996-12-26 2016-12-26 US US6037157 Yes 1996-12-26 2016-12-26 US US6232333 Yes 1998-05-07 2018-05-07 US US7432294 Yes 2000-11-22 2020-11-22 US US7141593 Yes 2000-11-22 2020-11-22 US US5914332 Yes 1996-06-13 2016-06-13 US US6284767 Yes 1996-08-15 2016-08-15 US US7364752 Yes 2001-05-10 2021-05-10 US US8309613 Yes 2005-06-24 2025-06-24 US US8377952 Yes 2008-04-22 2028-04-22 US US8691878 Yes 2005-02-25 2025-02-25 US US8025899 Yes 2008-06-14 2028-06-14 US US7148359 Yes 2000-01-19 2020-01-19 US US8470347 Yes 2007-03-17 2027-03-17 US US8268349 Yes 2005-02-25 2025-02-25 US US8399015 Yes 2005-02-25 2025-02-25 US US6458818 Yes 1998-05-07 2018-05-07 US US6521651 Yes 1998-05-07 2018-05-07 US US6911214 Yes 2002-05-28 2022-05-28 US US8501219 No 2001-11-28 2021-11-28 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.00192 mg/mL ALOGPS logP 3.91 ALOGPS logP 4.69 ChemAxon logS -5.5 ALOGPS pKa (Strongest Acidic) 13.39 ChemAxon pKa (Strongest Basic) -1.5 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 5 ChemAxon Hydrogen Donor Count 4 ChemAxon Polar Surface Area 120 Å2 ChemAxon Rotatable Bond Count 15 ChemAxon Refractivity 179.36 m3·mol-1 ChemAxon Polarizability 69.2 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 - 0.6593 Blood Brain Barrier - 0.9916 Caco-2 permeable + 0.8856 P-glycoprotein substrate Substrate 0.8755 P-glycoprotein inhibitor I Inhibitor 0.7355 P-glycoprotein inhibitor II Inhibitor 0.5277 Renal organic cation transporter Non-inhibitor 0.8578 CYP450 2C9 substrate Non-substrate 0.7508 CYP450 2D6 substrate Non-substrate 0.9116 CYP450 3A4 substrate Substrate 0.6732 CYP450 1A2 substrate Non-inhibitor 0.8935 CYP450 2C9 inhibitor Non-inhibitor 0.7326 CYP450 2D6 inhibitor Non-inhibitor 0.9438 CYP450 2C19 inhibitor Non-inhibitor 0.7983 CYP450 3A4 inhibitor Non-inhibitor 0.6469 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9054 Ames test Non AMES toxic 0.8049 Carcinogenicity Non-carcinogens 0.7865 Biodegradation Not ready biodegradable 0.9182 Rat acute toxicity 2.2503 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.8605 hERG inhibition (predictor II) Inhibitor 0.8475
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available 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 MS/MS Spectrum - , positive LC-MS/MS splash10-0fb9-0119005000-e99616dc321beea979ae MS/MS Spectrum - , positive LC-MS/MS splash10-0532-1900601000-f85a252f1640f27563a8
Taxonomy
- Description
- This compound belongs to the class of organic compounds known as valine and derivatives. These are compounds containing valine or a derivative thereof resulting from reaction of valine at the amino group or the carboxy group, or from the replacement of any hydrogen of glycine by a heteroatom.
- Kingdom
- Organic compounds
- Super Class
- Organic acids and derivatives
- Class
- Carboxylic acids and derivatives
- Sub Class
- Amino acids, peptides, and analogues
- Direct Parent
- Valine and derivatives
- Alternative Parents
- Amphetamines and derivatives / m-Xylenes / Phenol ethers / Phenoxy compounds / Alkyl aryl ethers / Pyrimidones / Diazinanes / N-acyl amines / Secondary carboxylic acid amides / Ureas show 7 more
- Substituents
- Valine or derivatives / Amphetamine or derivatives / Phenoxy compound / Phenol ether / M-xylene / Xylene / Alkyl aryl ether / Pyrimidone / Monocyclic benzene moiety / 1,3-diazinane show 23 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- dicarboxylic acid diamide, amphetamines (CHEBI:31781)
Targets
- Kind
- Protein
- Organism
- Human immunodeficiency virus 1
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Aspartic-type endopeptidase activity
- Specific Function
- Not Available
- Gene Name
- pol
- Uniprot ID
- Q72874
- Uniprot Name
- Pol polyprotein
- Molecular Weight
- 10778.7 Da
References
- Garriga C, Perez-Elias MJ, Delgado R, Ruiz L, Najera R, Pumarola T, Alonso-Socas Mdel M, Garcia-Bujalance S, Menendez-Arias L: Mutational patterns and correlated amino acid substitutions in the HIV-1 protease after virological failure to nelfinavir- and lopinavir/ritonavir-based treatments. J Med Virol. 2007 Nov;79(11):1617-28. [PubMed:17854027]
- Reddy GS, Ali A, Nalam MN, Anjum SG, Cao H, Nathans RS, Schiffer CA, Rana TM: Design and synthesis of HIV-1 protease inhibitors incorporating oxazolidinones as P2/P2' ligands in pseudosymmetric dipeptide isosteres. J Med Chem. 2007 Sep 6;50(18):4316-28. Epub 2007 Aug 16. [PubMed:17696512]
- Wittayanarakul K, Hannongbua S, Feig M: Accurate prediction of protonation state as a prerequisite for reliable MM-PB(GB)SA binding free energy calculations of HIV-1 protease inhibitors. J Comput Chem. 2008 Apr 15;29(5):673-85. [PubMed:17849388]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
- Authors unspecified: Lopinavir/ritonavir: a protease inhibitor combination. Med Lett Drugs Ther. 2001 Jan 8;43(1095):1-2. [PubMed:11151088]
Enzymes
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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
- Lopez Aspiroz E, Cabrera Figueroa SE, Iglesias Gomez A, Valverde Merino MP, Dominguez-Gil Hurle A: CYP3A4 polymorphism and lopinavir toxicity in an HIV-infected pregnant woman. Clin Drug Investig. 2015 Jan;35(1):61-6. doi: 10.1007/s40261-014-0245-7. [PubMed:25391550]
- Zhou SF: Drugs behave as substrates, inhibitors and inducers of human cytochrome P450 3A4. Curr Drug Metab. 2008 May;9(4):310-22. [PubMed:18473749]
- Yeh RF, Gaver VE, Patterson KB, Rezk NL, Baxter-Meheux F, Blake MJ, Eron JJ Jr, Klein CE, Rublein JC, Kashuba AD: Lopinavir/ritonavir induces the hepatic activity of cytochrome P450 enzymes CYP2C9, CYP2C19, and CYP1A2 but inhibits the hepatic and intestinal activity of CYP3A as measured by a phenotyping drug cocktail in healthy volunteers. J Acquir Immune Defic Syndr. 2006 May;42(1):52-60. doi: 10.1097/01.qai.0000219774.20174.64. [PubMed:16639344]
- Weemhoff JL, von Moltke LL, Richert C, Hesse LM, Harmatz JS, Greenblatt DJ: Apparent mechanism-based inhibition of human CYP3A in-vitro by lopinavir. J Pharm Pharmacol. 2003 Mar;55(3):381-6. doi: 10.1211/002235702739. [PubMed:12724045]
- Sham HL, Betebenner DA, Herrin T, Kumar G, Saldivar A, Vasavanonda S, Molla A, Kempf DJ, Plattner JJ, Norbeck DW: Synthesis and antiviral activities of the major metabolites of the HIV protease inhibitor ABT-378 (Lopinavir). Bioorg Med Chem Lett. 2001 Jun 4;11(11):1351-3. [PubMed:11378352]
- Drug Interactions & Labeling - FDA [Link]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- 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
References
- Weemhoff JL, von Moltke LL, Richert C, Hesse LM, Harmatz JS, Greenblatt DJ: Apparent mechanism-based inhibition of human CYP3A in-vitro by lopinavir. J Pharm Pharmacol. 2003 Mar;55(3):381-6. doi: 10.1211/002235702739. [PubMed:12724045]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- 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
- Weemhoff JL, von Moltke LL, Richert C, Hesse LM, Harmatz JS, Greenblatt DJ: Apparent mechanism-based inhibition of human CYP3A in-vitro by lopinavir. J Pharm Pharmacol. 2003 Mar;55(3):381-6. doi: 10.1211/002235702739. [PubMed:12724045]
- Kaletra, FDA label [File]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- 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
- CYP2B6
- Uniprot ID
- P20813
- Uniprot Name
- Cytochrome P450 2B6
- Molecular Weight
- 56277.81 Da
References
- Weemhoff JL, von Moltke LL, Richert C, Hesse LM, Harmatz JS, Greenblatt DJ: Apparent mechanism-based inhibition of human CYP3A in-vitro by lopinavir. J Pharm Pharmacol. 2003 Mar;55(3):381-6. doi: 10.1211/002235702739. [PubMed:12724045]
- Kind
- Protein
- Organism
- Human
- 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
- Weemhoff JL, von Moltke LL, Richert C, Hesse LM, Harmatz JS, Greenblatt DJ: Apparent mechanism-based inhibition of human CYP3A in-vitro by lopinavir. J Pharm Pharmacol. 2003 Mar;55(3):381-6. doi: 10.1211/002235702739. [PubMed:12724045]
- Hughes CA, Freitas A, Miedzinski LJ: Interaction between lopinavir/ritonavir and warfarin. CMAJ. 2007 Aug 14;177(4):357-9. doi: 10.1503/cmaj.061284. [PubMed:17698824]
- Lim ML, Min SS, Eron JJ, Bertz RJ, Robinson M, Gaedigk A, Kashuba AD: Coadministration of lopinavir/ritonavir and phenytoin results in two-way drug interaction through cytochrome P-450 induction. J Acquir Immune Defic Syndr. 2004 Aug 15;36(5):1034-40. [PubMed:15247556]
- Kaletra FDA label [File]
- Cytochrome P450 Enzymes and Transporters Induced by Anti-Human Immunodeficiency Virus Protease Inhibitors in Human Hepatocytes: Implications for Predicting Clinical Drug Interactions [File]
- Kaletra EPAR [File]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- 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 group
- Organism
- Human
- Pharmacological action
- No
- 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...
Components:
| Name | UniProt ID |
|---|---|
| Cytochrome P450 3A4 | P08684 |
| Cytochrome P450 3A43 | Q9HB55 |
| Cytochrome P450 3A5 | P20815 |
| Cytochrome P450 3A7 | P24462 |
References
- Drug Interactions & Labeling - FDA [Link]
Transporters
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- 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
References
- Vishnuvardhan D, Moltke LL, Richert C, Greenblatt DJ: Lopinavir: acute exposure inhibits P-glycoprotein; extended exposure induces P-glycoprotein. AIDS. 2003 May 2;17(7):1092-4. [PubMed:12700464]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- 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
References
- Annaert P, Ye ZW, Stieger B, Augustijns P: Interaction of HIV protease inhibitors with OATP1B1, 1B3, and 2B1. Xenobiotica. 2010 Mar;40(3):163-76. doi: 10.3109/00498250903509375. [PubMed:20102298]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- 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
References
- FDA Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers [Link]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- No
- Actions
- Substrate
- 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
References
- Pedersen JM, Matsson P, Bergstrom CA, Hoogstraate J, Noren A, LeCluyse EL, Artursson P: Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43. doi: 10.1093/toxsci/kft197. Epub 2013 Sep 6. [PubMed:24014644]
Drug created on August 29, 2007 12:45 / Updated on October 16, 2018 16:04