Clobazam
Product: Farampator
Identifier : DBSNPE000133
Drug : DB00349 (Clobazam)
Interacting Gene/Enzyme : Cytochrome P450 2C19
Gene Name : CYP2C19
UniProt ID : P33261
Allele Name : CYP2C19*2
Genotype(s) : (A;A) / (A;G)
Type(s) : ADR Directly Studied
Groups : Non-functional CYP2C19
Description : Clobazem is metabolized into N-desmethylclobazem (NCLB) mostly by CYP3A4. NCLB is primarily metabolized by 2C19. Those with one 2C19*2 allele mutation (1*/2*) are intermediate metabolizers of NCLB. Those with two (2*/2*) mutations will metabolize NCLB poorly in comparisone to extensive metabolizers (1*/1*). Levels of NCLB can be five times higher in poor metabolizers, and two times higher in intermediate metabolizers as compared to individuals who are extensive metabolizers. The safety and efficacy of clobazem may be affected by polymorphic expression of CYP2C19*2.
References :
- Giraud C, Tran A, Rey E, Vincent J, Treluyer JM, Pons G: In vidivo characterization of clobazam metabolism by recombinant cytochrome P450 enzymes: importance of CYP2C19. Drug Metab Dispos. 2004 Nov;32(11):1279-86. [PubMed:15483195 ]
PMID: 21622856
Clobazam
Product: A-803468
Identifier : DBSNPE006010
Drug : DB00349 (Clobazam)
Interacting Gene/Enzyme : Cytochrome P450 2C19
Gene Name : CYP2C19
UniProt ID : P33261
Allele Name : CYP2C19*2A
Genotype(s) : Not Available
Type(s) : ADR Inferred
Groups : Non-functional CYP2C19
Description : Clobazem is metabolized into N-desmethylclobazem (NCLB) mostly by CYP3A4. NCLB is primarily metabolized by 2C19. Those with one 2C19*2 allele mutation (1*/2*) are intermediate metabolizers of NCLB. Those with two (2*/2*) mutations will metabolize NCLB poorly in comparisone to extensive metabolizers (1*/1*). Levels of NCLB can be five times higher in poor metabolizers, and two times higher in intermediate metabolizers as compared to individuals who are extensive metabolizers. The safety and efficacy of clobazem may be affected by polymorphic expression of CYP2C19*2.
References :
- de Morais SM, Wilkinson GR, Blaisdell J, Nakamura K, Meyer UA, Goldstein JA: The major genetic defect responsible for the polymorphism of S-mephenytoin metabolism in humans. J Biol Chem. 1994 Jun 3;269(22):15419-22. [PubMed:8195181 ]
- Fukushima-Uesaka H, Saito Y, Maekawa K, Ozawa S, Hasegawa R, Kajio H, Kuzuya N, Yasuda K, Kawamoto M, Kamatani N, Suzuki K, Yanagawa T, Tohkin M, Sawada J: Genetic variations and haplotypes of CYP2C19 in a Japanese population. Drug Metab Pharmacokinet. 2005 Aug;20(4):300-7. [PubMed:16141610 ]
- Lee SJ, Kim WY, Kim H, Shon JH, Lee SS, Shin JG: Identification of new CYP2C19 variants exhibiting decreased enzyme activity in the metabolism of S-mephenytoin and omeprazole. Drug Metab Dispos. 2009 Nov;37(11):2262-9. doi: 10.1124/dmd.109.028175. Epub 2009 Aug 6. [PubMed:19661214 ]
- The Human Cytochrome P450 (CYP) Allele Nomenclature Database [Link]
PMID: 10942519
Clobazam
Product: GSK2636772
Identifier : DBSNPE006011
Drug : DB00349 (Clobazam)
Interacting Gene/Enzyme : Cytochrome P450 2C19
Gene Name : CYP2C19
UniProt ID : P33261
Allele Name : CYP2C19*2B
Genotype(s) : Not Available
Type(s) : ADR Inferred
Groups : Non-functional CYP2C19
Description : Clobazem is metabolized into N-desmethylclobazem (NCLB) mostly by CYP3A4. NCLB is primarily metabolized by 2C19. Those with one 2C19*2 allele mutation (1*/2*) are intermediate metabolizers of NCLB. Those with two (2*/2*) mutations will metabolize NCLB poorly in comparisone to extensive metabolizers (1*/1*). Levels of NCLB can be five times higher in poor metabolizers, and two times higher in intermediate metabolizers as compared to individuals who are extensive metabolizers. The safety and efficacy of clobazem may be affected by polymorphic expression of CYP2C19*2.
References :
- Ibeanu GC, Goldstein JA, Meyer U, Benhamou S, Bouchardy C, Dayer P, Ghanayem BI, Blaisdell J: Identification of new human CYP2C19 alleles (CYP2C19*6 and CYP2C19*2B) in a Caucasian poor metabolizer of mephenytoin. J Pharmacol Exp Ther. 1998 Sep;286(3):1490-5. [PubMed:9732415 ]
- The Human Cytochrome P450 (CYP) Allele Nomenclature Database [Link]
PMID: 10723137
Clobazam
Product: TAK-439
Identifier : DBSNPE006012
Drug : DB00349 (Clobazam)
Interacting Gene/Enzyme : Cytochrome P450 2C19
Gene Name : CYP2C19
UniProt ID : P33261
Allele Name : CYP2C19*3
Genotype(s) : Not Available
Type(s) : ADR Inferred
Groups : Non-functional CYP2C19
Description : Clobazem is metabolized into N-desmethylclobazem (NCLB) mostly by CYP3A4. NCLB is primarily metabolized by 2C19. Those with one 2C19*2 allele mutation (1*/2*) are intermediate metabolizers of NCLB. Those with two (2*/2*) mutations will metabolize NCLB poorly in comparisone to extensive metabolizers (1*/1*). Levels of NCLB can be five times higher in poor metabolizers, and two times higher in intermediate metabolizers as compared to individuals who are extensive metabolizers. The safety and efficacy of clobazem may be affected by polymorphic expression of CYP2C19*2.
References :
- De Morais SM, Wilkinson GR, Blaisdell J, Meyer UA, Nakamura K, Goldstein JA: Identification of a new genetic defect responsible for the polymorphism of (S)-mephenytoin metabolism in Japanese. Mol Pharmacol. 1994 Oct;46(4):594-8. [PubMed:7969038 ]
- Fukushima-Uesaka H, Saito Y, Maekawa K, Ozawa S, Hasegawa R, Kajio H, Kuzuya N, Yasuda K, Kawamoto M, Kamatani N, Suzuki K, Yanagawa T, Tohkin M, Sawada J: Genetic variations and haplotypes of CYP2C19 in a Japanese population. Drug Metab Pharmacokinet. 2005 Aug;20(4):300-7. [PubMed:16141610 ]
- The Human Cytochrome P450 (CYP) Allele Nomenclature Database [Link]
PMID: 18690793
Clobazam
Product: MBX-2983
Identifier : DBSNPE006013
Drug : DB00349 (Clobazam)
Interacting Gene/Enzyme : Cytochrome P450 2C19
Gene Name : CYP2C19
UniProt ID : P33261
Allele Name : CYP2C19*4
Genotype(s) : Not Available
Type(s) : ADR Inferred
Groups : Non-functional CYP2C19
Description : Clobazem is metabolized into N-desmethylclobazem (NCLB) mostly by CYP3A4. NCLB is primarily metabolized by 2C19. Those with one 2C19*2 allele mutation (1*/2*) are intermediate metabolizers of NCLB. Those with two (2*/2*) mutations will metabolize NCLB poorly in comparisone to extensive metabolizers (1*/1*). Levels of NCLB can be five times higher in poor metabolizers, and two times higher in intermediate metabolizers as compared to individuals who are extensive metabolizers. The safety and efficacy of clobazem may be affected by polymorphic expression of CYP2C19*2.
References :
- Ferguson RJ, De Morais SM, Benhamou S, Bouchardy C, Blaisdell J, Ibeanu G, Wilkinson GR, Sarich TC, Wright JM, Dayer P, Goldstein JA: A new genetic defect in human CYP2C19: mutation of the initiation codon is responsible for poor metabolism of S-mephenytoin. J Pharmacol Exp Ther. 1998 Jan;284(1):356-61. [PubMed:9435198 ]
- Scott SA, Martis S, Peter I, Kasai Y, Kornreich R, Desnick RJ: Identification of CYP2C19*4B: pharmacogenetic implications for drug metabolism including clopidogrel responsiveness. Pharmacogenomics J. 2012 Aug;12(4):297-305. doi: 10.1038/tpj.2011.5. Epub 2011 Mar 1. [PubMed:21358751 ]
- Zackrisson AL, Lindblom B, Ahlner J: High frequency of occurrence of CYP2D6 gene duplication/multiduplication indicating uldivarapid metabolism among suicide cases. Clin Pharmacol Ther. 2010 Sep;88(3):354-9. doi: 10.1038/clpt.2009.216. Epub 2009 Nov 11. [PubMed:19907421 ]
- The Human Cytochrome P450 (CYP) Allele Nomenclature Database [Link]
PMID: 11753686
Clobazam
Product: Indacaterol
Identifier : DBSNPE006014
Drug : DB00349 (Clobazam)
Interacting Gene/Enzyme : Cytochrome P450 2C19
Gene Name : CYP2C19
UniProt ID : P33261
Allele Name : CYP2C19*5
Genotype(s) : Not Available
Type(s) : ADR Inferred
Groups : Non-functional CYP2C19
Description : Clobazem is metabolized into N-desmethylclobazem (NCLB) mostly by CYP3A4. NCLB is primarily metabolized by 2C19. Those with one 2C19*2 allele mutation (1*/2*) are intermediate metabolizers of NCLB. Those with two (2*/2*) mutations will metabolize NCLB poorly in comparisone to extensive metabolizers (1*/1*). Levels of NCLB can be five times higher in poor metabolizers, and two times higher in intermediate metabolizers as compared to individuals who are extensive metabolizers. The safety and efficacy of clobazem may be affected by polymorphic expression of CYP2C19*2.
References :
- Xiao ZS, Goldstein JA, Xie HG, Blaisdell J, Wang W, Jiang CH, Yan FX, He N, Huang SL, Xu ZH, Zhou HH: Differences in the incidence of the CYP2C19 polymorphism affecting the S-mephenytoin phenotype in Chinese Han and Bai populations and identification of a new rare CYP2C19 mutant allele. J Pharmacol Exp Ther. 1997 Apr;281(1):604-9. [PubMed:9103550 ]
- Ibeanu GC, Blaisdell J, Ghanayem BI, Beyeler C, Benhamou S, Bouchardy C, Wilkinson GR, Dayer P, Daly AK, Goldstein JA: An additional defective allele, CYP2C19*5, condivibutes to the S-mephenytoin poor metabolizer phenotype in Caucasians. Pharmacogenetics. 1998 Apr;8(2):129-35. [PubMed:10022751 ]
- The Human Cytochrome P450 (CYP) Allele Nomenclature Database [Link]
PMID: 7720709
Clobazam
Product: Episilvestrol
Identifier : DBSNPE006015
Drug : DB00349 (Clobazam)
Interacting Gene/Enzyme : Cytochrome P450 2C19
Gene Name : CYP2C19
UniProt ID : P33261
Allele Name : CYP2C19*6
Genotype(s) : Not Available
Type(s) : ADR Inferred
Groups : Non-functional CYP2C19
Description : Clobazem is metabolized into N-desmethylclobazem (NCLB) mostly by CYP3A4. NCLB is primarily metabolized by 2C19. Those with one 2C19*2 allele mutation (1*/2*) are intermediate metabolizers of NCLB. Those with two (2*/2*) mutations will metabolize NCLB poorly in comparisone to extensive metabolizers (1*/1*). Levels of NCLB can be five times higher in poor metabolizers, and two times higher in intermediate metabolizers as compared to individuals who are extensive metabolizers. The safety and efficacy of clobazem may be affected by polymorphic expression of CYP2C19*2.
References :
- Ibeanu GC, Goldstein JA, Meyer U, Benhamou S, Bouchardy C, Dayer P, Ghanayem BI, Blaisdell J: Identification of new human CYP2C19 alleles (CYP2C19*6 and CYP2C19*2B) in a Caucasian poor metabolizer of mephenytoin. J Pharmacol Exp Ther. 1998 Sep;286(3):1490-5. [PubMed:9732415 ]
- The Human Cytochrome P450 (CYP) Allele Nomenclature Database [Link]
PMID: 23364809
Clobazam
Product: Agomelatine
Identifier : DBSNPE006016
Drug : DB00349 (Clobazam)
Interacting Gene/Enzyme : Cytochrome P450 2C19
Gene Name : CYP2C19
UniProt ID : P33261
Allele Name : CYP2C19*7
Genotype(s) : Not Available
Type(s) : ADR Inferred
Groups : Non-functional CYP2C19
Description : Clobazem is metabolized into N-desmethylclobazem (NCLB) mostly by CYP3A4. NCLB is primarily metabolized by 2C19. Those with one 2C19*2 allele mutation (1*/2*) are intermediate metabolizers of NCLB. Those with two (2*/2*) mutations will metabolize NCLB poorly in comparisone to extensive metabolizers (1*/1*). Levels of NCLB can be five times higher in poor metabolizers, and two times higher in intermediate metabolizers as compared to individuals who are extensive metabolizers. The safety and efficacy of clobazem may be affected by polymorphic expression of CYP2C19*2.
References :
- Ibeanu GC, Blaisdell J, Ferguson RJ, Ghanayem BI, Brosen K, Benhamou S, Bouchardy C, Wilkinson GR, Dayer P, Goldstein JA: A novel divansversion in the indivon 5 donor splice junction of CYP2C19 and a sequence polymorphism in exon 3 condivibute to the poor metabolizer phenotype for the anticonvulsant drug S-mephenytoin. J Pharmacol Exp Ther. 1999 Aug;290(2):635-40. [PubMed:10411572 ]
- The Human Cytochrome P450 (CYP) Allele Nomenclature Database [Link]
PMID: 10640519
Clobazam
Product: Cobicistat
Identifier : DBSNPE006017
Drug : DB00349 (Clobazam)
Interacting Gene/Enzyme : Cytochrome P450 2C19
Gene Name : CYP2C19
UniProt ID : P33261
Defining Change(s) :
- 557G>C (rs140278421 )
- 991A>G
Allele Name : CYP2C19*22
Genotype(s) : Not Available
Type(s) : ADR Inferred
Groups : Non-functional CYP2C19
Description : Clobazem is metabolized into N-desmethylclobazem (NCLB) mostly by CYP3A4. NCLB is primarily metabolized by 2C19. Those with one 2C19*2 allele mutation (1*/2*) are intermediate metabolizers of NCLB. Those with two (2*/2*) mutations will metabolize NCLB poorly in comparisone to extensive metabolizers (1*/1*). Levels of NCLB can be five times higher in poor metabolizers, and two times higher in intermediate metabolizers as compared to individuals who are extensive metabolizers. The safety and efficacy of clobazem may be affected by polymorphic expression of CYP2C19*2.
References :
- Takahashi M, Saito T, Ito M, Tsukada C, Katono Y, Hosono H, Maekawa M, Shimada M, Mano N, Oda A, Hirasawa N, Hiratsuka M: Functional characterization of 21 CYP2C19 allelic variants for clopidogrel 2-oxidation. Pharmacogenomics J. 2015 Feb;15(1):26-32. doi: 10.1038/tpj.2014.30. Epub 2014 Jul 8. [PubMed:25001882 ]
- The Human Cytochrome P450 (CYP) Allele Nomenclature Database [Link]
PMID: 10706389
Clobazam
Product: BAY 80-6947
Identifier : DBSNPE006018
Drug : DB00349 (Clobazam)
Interacting Gene/Enzyme : Cytochrome P450 2C19
Gene Name : CYP2C19
UniProt ID : P33261
Defining Change(s) :
- 99C>T (rs17885098 )
- 991A>G (rs3758581 )
- 1004G>A (rs118203757 )
- 1197A>G
Allele Name : CYP2C19*24
Genotype(s) : Not Available
Type(s) : ADR Inferred
Groups : Non-functional CYP2C19
Description : Clobazem is metabolized into N-desmethylclobazem (NCLB) mostly by CYP3A4. NCLB is primarily metabolized by 2C19. Those with one 2C19*2 allele mutation (1*/2*) are intermediate metabolizers of NCLB. Those with two (2*/2*) mutations will metabolize NCLB poorly in comparisone to extensive metabolizers (1*/1*). Levels of NCLB can be five times higher in poor metabolizers, and two times higher in intermediate metabolizers as compared to individuals who are extensive metabolizers. The safety and efficacy of clobazem may be affected by polymorphic expression of CYP2C19*2.
References :
- Zhou Q, Yu XM, Lin HB, Wang L, Yun QZ, Hu SN, Wang DM: Genetic polymorphism, linkage disequilibrium, haplotype sdivucture and novel allele analysis of CYP2C19 and CYP2D6 in Han Chinese. Pharmacogenomics J. 2009 Dec;9(6):380-94. doi: 10.1038/tpj.2009.31. Epub 2009 Jul 28. [PubMed:19636337 ]
- The Human Cytochrome P450 (CYP) Allele Nomenclature Database [Link]
PMID: 10448131
Clobazam
Product: Naphthoquine (phosphate)
Identifier : DBSNPE006019
Drug : DB00349 (Clobazam)
Interacting Gene/Enzyme : Cytochrome P450 2C19
Gene Name : CYP2C19
UniProt ID : P33261
Allele Name : CYP2C19*35
Genotype(s) : Not Available
Type(s) : ADR Inferred
Groups : Non-functional CYP2C19
Description : Clobazem is metabolized into N-desmethylclobazem (NCLB) mostly by CYP3A4. NCLB is primarily metabolized by 2C19. Those with one 2C19*2 allele mutation (1*/2*) are intermediate metabolizers of NCLB. Those with two (2*/2*) mutations will metabolize NCLB poorly in comparisone to extensive metabolizers (1*/1*). Levels of NCLB can be five times higher in poor metabolizers, and two times higher in intermediate metabolizers as compared to individuals who are extensive metabolizers. The safety and efficacy of clobazem may be affected by polymorphic expression of CYP2C19*2.
References :
- Chaudhry AS, Prasad B, Shirasaka Y, Fohner A, Finkelstein D, Fan Y, Wang S, Wu G, Aklillu E, Sim SC, Thummel KE, Schuetz EG: The CYP2C19 Indivon 2 Branch Point SNP is the Ancesdival Polymorphism Condivibuting to the Poor Metabolizer Phenotype in Livers with CYP2C19*35 and CYP2C19*2 Alleles. Drug Metab Dispos. 2015 Aug;43(8):1226-35. doi: 10.1124/dmd.115.064428. Epub 2015 May 28. [PubMed:26021325 ]
- The Human Cytochrome P450 (CYP) Allele Nomenclature Database [Link]
PMID: 26634247