Identification
- Summary
Trabectedin is an alkylating agent approved for the treatment of unresectable or metastatic soft tissue sarcoma (liposarcoma or leiomyosarcoma).
- Brand Names
- Yondelis
- Generic Name
- Trabectedin
- DrugBank Accession Number
- DB05109
- Background
Trabectedin, also referred as ET-743 during its development, is a marine-derived antitumor agent discovered in the Carribean tunicate Ecteinascidia turbinata and now produced synthetically. Trabectedin has a unique mechanism of action. It binds to the minor groove of DNA interfering with cell division and genetic transcription processes and DNA repair machinery. It is approved for use in Europe, Russia and South Korea for the treatment of advanced soft tissue sarcoma. It is currently under evaluation for the treatment of breast cancer, prostate cancer, in addition to pediatric sarcomas. Both the European Commission and the U.S. Food and Drug Administration (FDA) have approved trabectedin as an orphan drug in soft tissue sarcomas and ovarian cancer. On October 23, 2015, the FDA approved trabectedin, (as Yondelis), for the treatment of specific soft tissue sarcomas.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Trabectedin (DB05109)
- Weight
- Average: 761.837
Monoisotopic: 761.261829923 - Chemical Formula
- C39H43N3O11S
- Synonyms
- Ecteinascidin 743
- Trabectedin
- Trabectedina
- External IDs
- ET-743
- NSC 684766
- NSC-648766
Pharmacology
- Indication
Indicated for treatment of advanced soft tissue sarcoma in patients refractory to or unsuitable to receive anthracycline or ifosfamide chemotherapy in Europe, Russia and South Korea. Approved for orphan drug status by the U.S. FDA for treatment of soft tissue sarcomas and ovarian cancer. Investigated for use/treatment in cancer/tumors (unspecified), gastric cancer, ovarian cancer, pediatric indications, sarcoma, and solid tumors.
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
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Metastatic leiomyosarcoma •••••••••••• Treatment of Metastatic liposarcoma •••••••••••• Used in combination to treat Relapsed platinum-sensitive ovarian cancer Regimen in combination with: Doxorubicin (DB00997) •••••••••••• Treatment of Unresectable leiomyosarcoma •••••••••••• Treatment of Unresectable liposarcoma •••••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Two of the rings in the drug's structure allows it to covalently bind to the minor groove of DNA. The third ring protrudes from the DNA which lets it interact with nearby nuclear proteins. This has the additive effect of blocking cell division at the G2 phase.
- Mechanism of action
Trabectedin interacts with the minor groove of DNA and alkylates guanine at the N2 position, which bends towards the major groove. In this manner, it is thought that the drug affects various transcription factors involved in cell proliferation, particularly via the transcription-coupled nucleotide excision repair system. Trabectedin blocks the cell cycle at the G2 phase, while cells at the G1 phase are most sensitive to the drug. It also inhibits overexpression of the multidrug resistance-1 gene (MDR-1) coding for the P-glycoprotein that is a major factor responsible for cells developing resistance to cancer drugs. The agent is also thought to interfere with the nucleotide excision repair pathways of cancer cells, suggesting that it could be effective in the treatment of many cancer types including melanoma and sarcoma, as well as lung, breast, ovarian, endometrial and prostate cancers; clinical evaluations are underway in these indications.
Target Actions Organism ADNA binderHumans - Absorption
Administered intravenously.
- Volume of distribution
Not Available
- Protein binding
94 to 98%
- Metabolism
Hover over products below to view reaction partners
- Route of elimination
Not Available
- Half-life
33-50 hours
- Clearance
Not Available
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
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 softwareAbametapir The serum concentration of Trabectedin can be increased when it is combined with Abametapir. Abatacept The metabolism of Trabectedin can be increased when combined with Abatacept. Abciximab The risk or severity of bleeding can be increased when Abciximab is combined with Trabectedin. Abiraterone The metabolism of Trabectedin can be decreased when combined with Abiraterone. Abrocitinib The metabolism of Abrocitinib can be decreased when combined with Trabectedin. - Food Interactions
- Avoid alcohol. There may be an additive hepatotoxic effect if alcohol and trabectedin are coadministered.
- Avoid St. John's Wort. This herb induces CYP3A4 metabolism, which may reduce the serum concentration of trabectedin.
- Exercise caution with grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase the serum concentration of trabectedin.
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 Yondelis Powder, for solution 1 mg / vial Intravenous Valeo Pharma Corp. 2010-08-05 Not applicable Canada 
Yondelis Injection, powder, for solution 1 mg Intravenous Pharma Mar 2020-12-16 Not applicable EU 
Yondelis Injection, powder, lyophilized, for solution 0.05 mg/1mL Intravenous Janssen Products, LP 2015-10-23 Not applicable US 
Yondelis Injection, powder, for solution 0.25 mg Intravenous Pharma Mar 2020-12-16 Not applicable EU
Categories
- ATC Codes
- L01CX01 — Trabectedin
- Drug Categories
- Agents Causing Muscle Toxicity
- Alkylating Activity
- Alkylating Drugs
- Antineoplastic Agents
- Antineoplastic Agents, Alkylating
- Antineoplastic and Immunomodulating Agents
- Cytochrome P-450 CYP2C19 Substrates
- Cytochrome P-450 CYP2C19 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 CYP2C9 Substrates
- Cytochrome P-450 CYP2C9 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP2D6 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 CYP2E1 Substrates
- Cytochrome P-450 CYP2E1 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A4 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 Substrates
- Dioxoles
- Heterocyclic Compounds, Fused-Ring
- Immunosuppressive Agents
- Isoquinolines
- Myelosuppressive Agents
- Narrow Therapeutic Index Drugs
- Noxae
- Tetrahydroisoquinolines
- Toxic Actions
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as benzazocines. These are organic compounds containing the benzazocine ring system, which consists of a benzene ring bound to an azocine ring.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Benzene and substituted derivatives
- Sub Class
- Benzazocines
- Direct Parent
- Benzazocines
- Alternative Parents
- Tetrahydroisoquinolines / Alpha amino acids and derivatives / Benzodioxoles / Anisoles / 1-hydroxy-2-unsubstituted benzenoids / 1-hydroxy-4-unsubstituted benzenoids / Alkyl aryl ethers / N-methylpiperazines / Aralkylamines / Dicarboxylic acids and derivatives show 14 more
- Substituents
- 1,4-diazinane / 1-hydroxy-2-unsubstituted benzenoid / 1-hydroxy-4-unsubstituted benzenoid / Acetal / Alkanolamine / Alkyl aryl ether / Alpha-amino acid or derivatives / Amine / Amino acid or derivatives / Anisole show 32 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- tertiary amino compound, acetate ester, polyphenol, organic sulfide, bridged compound, isoquinoline alkaloid, hemiaminal, lactone, azaspiro compound, organic heteropolycyclic compound, oxaspiro compound (CHEBI:84050)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- ID0YZQ2TCP
- CAS number
- 114899-77-3
- InChI Key
- PKVRCIRHQMSYJX-AIFWHQITSA-N
- InChI
- InChI=1S/C39H43N3O11S/c1-16-9-20-10-22-37(46)42-23-13-50-38(47)39(21-12-25(48-5)24(44)11-19(21)7-8-40-39)14-54-36(30(42)29(41(22)4)26(20)31(45)32(16)49-6)28-27(23)35-34(51-15-52-35)17(2)33(28)53-18(3)43/h9,11-12,22-23,29-30,36-37,40,44-46H,7-8,10,13-15H2,1-6H3/t22-,23-,29+,30+,36+,37-,39+/m0/s1
- IUPAC Name
- (1R,2R,3R,11S,12S,14R,26R)-5,6',12-trihydroxy-6,7'-dimethoxy-7,21,30-trimethyl-27-oxo-3',4'-dihydro-2'H-17,19,28-trioxa-24-thia-13,30-diazaspiro[heptacyclo[12.9.6.1^{3,11}.0^{2,13}.0^{4,9}.0^{15,23}.0^{16,20}]triacontane-26,1'-isoquinoline]-4,6,8,15,20,22-hexaen-22-yl acetate
- SMILES
- [H][C@@]12[C@@H]3SC[C@]4(NCCC5=C4C=C(OC)C(O)=C5)C(=O)OC[C@H](N1[C@@H](O)[C@@H]1CC4=CC(C)=C(OC)C(O)=C4[C@H]2N1C)C1=C2OCOC2=C(C)C(OC(C)=O)=C31
References
- Synthesis Reference
Elias J. Corey, David Gin, "Process for producing ecteinascidin compounds." U.S. Patent US5721362, issued December, 1995.
US5721362- General References
- Tavecchio M, Natoli C, Ubezio P, Erba E, D'Incalci M: Dynamics of cell cycle phase perturbations by trabectedin (ET-743) in nucleotide excision repair (NER)-deficient and NER-proficient cells, unravelled by a novel mathematical simulation approach. Cell Prolif. 2007 Dec;40(6):885-904. [Article]
- Krasner CN, McMeekin DS, Chan S, Braly PS, Renshaw FG, Kaye S, Provencher DM, Campos S, Gore ME: A Phase II study of trabectedin single agent in patients with recurrent ovarian cancer previously treated with platinum-based regimens. Br J Cancer. 2007 Dec 17;97(12):1618-24. Epub 2007 Nov 13. [Article]
- Carter NJ, Keam SJ: Trabectedin : a review of its use in the management of soft tissue sarcoma and ovarian cancer. Drugs. 2007;67(15):2257-76. [Article]
- Authors unspecified: Trabectedin: Ecteinascidin 743, Ecteinascidin-743, ET 743, ET-743, NSC 684766. Drugs R D. 2006;7(5):317-28. [Article]
- Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [Article]
- External Links
- Human Metabolome Database
- HMDB0015609
- PubChem Compound
- 108150
- PubChem Substance
- 99443229
- ChemSpider
- 97236
- 1716278
- ChEBI
- 84050
- ChEMBL
- CHEMBL450449
- ZINC
- ZINC000150338708
- PharmGKB
- PA165958349
- PDBe Ligand
- ECT
- Wikipedia
- Trabectedin
- FDA label
- Download (824 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 Completed Treatment Ovarian Cancer / Quality of Life (QOL) / Recurrent Ovarian Carcinoma 1 3 Active Not Recruiting Treatment Localized High-risk Soft Tissue Sarcomas of the Extremities and Trunk Wall in Adults 1 3 Completed Treatment Abdominal wall neoplasm / Fallopian Tube Neoplasms / Ovarian Neoplasms 1 3 Completed Treatment Advanced Liposarcoma or Leiomyosarcoma 1 3 Completed Treatment Advanced or Metastatic Liposarcoma or Leiomyosarcoma 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, powder, for solution Parenteral 0.25 mg Injection, powder, for solution Parenteral 1 mg Injection, powder, for solution 0.25 MG Injection, powder, for solution 1 MG Injection, powder, for solution Intravenous 0.25 MG Injection, powder, for solution Intravenous 1 MG Injection, powder, lyophilized, for solution Intravenous 0.05 mg/1mL Powder, for solution Intravenous 1 mg / vial Solution Intravenous 1.000 mg Injection, solution, concentrate Intravenous 1 mg Injection, powder, lyophilized, for solution Intravenous Injection, powder, for solution Intravenous 1.0 mg Injection, powder, lyophilized, for solution Intravenous 1 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA2428160 No 2009-10-13 2021-11-06 Canada CA2373794 No 2005-10-11 2020-05-15 Canada US8895557 Yes 2014-11-25 2028-07-07 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.328 mg/mL ALOGPS logP 2.04 ALOGPS logP 4.19 Chemaxon logS -3.4 ALOGPS pKa (Strongest Acidic) 9.26 Chemaxon pKa (Strongest Basic) 7.2 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 12 Chemaxon Hydrogen Donor Count 4 Chemaxon Polar Surface Area 168.72 Å2 Chemaxon Rotatable Bond Count 4 Chemaxon Refractivity 196.92 m3·mol-1 Chemaxon Polarizability 77.98 Å3 Chemaxon Number of Rings 9 Chemaxon Bioavailability 0 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption - 0.5216 Blood Brain Barrier - 0.9238 Caco-2 permeable - 0.6788 P-glycoprotein substrate Substrate 0.8988 P-glycoprotein inhibitor I Non-inhibitor 0.6957 P-glycoprotein inhibitor II Non-inhibitor 0.74 Renal organic cation transporter Non-inhibitor 0.8321 CYP450 2C9 substrate Non-substrate 0.8211 CYP450 2D6 substrate Non-substrate 0.7689 CYP450 3A4 substrate Substrate 0.6512 CYP450 1A2 substrate Non-inhibitor 0.804 CYP450 2C9 inhibitor Non-inhibitor 0.5287 CYP450 2D6 inhibitor Non-inhibitor 0.6514 CYP450 2C19 inhibitor Non-inhibitor 0.5436 CYP450 3A4 inhibitor Inhibitor 0.8832 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.6677 Ames test AMES toxic 0.9107 Carcinogenicity Non-carcinogens 0.8734 Biodegradation Not ready biodegradable 0.9782 Rat acute toxicity 2.6136 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9942 hERG inhibition (predictor II) Inhibitor 0.5329
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 268.9202408 predictedDarkChem Lite v0.1.0 [M-H]- 263.4573408 predictedDarkChem Lite v0.1.0 [M-H]- 246.56053 predictedDeepCCS 1.0 (2019) [M+H]+ 269.2515408 predictedDarkChem Lite v0.1.0 [M+H]+ 261.7799408 predictedDarkChem Lite v0.1.0 [M+H]+ 248.38542 predictedDeepCCS 1.0 (2019) [M+Na]+ 269.3608408 predictedDarkChem Lite v0.1.0 [M+Na]+ 261.9268408 predictedDarkChem Lite v0.1.0 [M+Na]+ 254.158 predictedDeepCCS 1.0 (2019)
Targets
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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Binder
References
- Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [Article]
- D'Incalci M, Galmarini CM: A review of trabectedin (ET-743): a unique mechanism of action. Mol Cancer Ther. 2010 Aug;9(8):2157-63. doi: 10.1158/1535-7163.MCT-10-0263. Epub 2010 Jul 20. [Article]
- Marco E, David-Cordonnier MH, Bailly C, Cuevas C, Gago F: Further insight into the DNA recognition mechanism of trabectedin from the differential affinity of its demethylated analogue ecteinascidin ET729 for the triplet DNA binding site CGA. J Med Chem. 2006 Nov 16;49(23):6925-9. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Prostaglandin-endoperoxide synthase activity
- Specific Function
- Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gas...
- Gene Name
- PTGS1
- Uniprot ID
- P23219
- Uniprot Name
- Prostaglandin G/H synthase 1
- Molecular Weight
- 68685.82 Da
References
- Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- 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
- Vermeir M, Hemeryck A, Cuyckens F, Francesch A, Bockx M, Van Houdt J, Steemans K, Mannens G, Aviles P, De Coster R: In vitro studies on the metabolism of trabectedin (YONDELIS) in monkey and man, including human CYP reaction phenotyping. Biochem Pharmacol. 2009 May 15;77(10):1642-54. doi: 10.1016/j.bcp.2009.02.020. Epub 2009 Mar 10. [Article]
- Brandon EF, Meijerman I, Klijn JS, den Arend D, Sparidans RW, Lazaro LL, Beijnen JH, Schellens JH: In-vitro cytotoxicity of ET-743 (Trabectedin, Yondelis), a marine anti-cancer drug, in the Hep G2 cell line: influence of cytochrome P450 and phase II inhibition, and cytochrome P450 induction. Anticancer Drugs. 2005 Oct;16(9):935-43. [Article]
- Machiels JP, Staddon A, Herremans C, Keung C, Bernard A, Phelps C, Khokhar NZ, Knoblauch R, Parekh TV, Dirix L, Sharma S: Impact of cytochrome P450 3A4 inducer and inhibitor on the pharmacokinetics of trabectedin in patients with advanced malignancies: open-label, multicenter studies. Cancer Chemother Pharmacol. 2014 Oct;74(4):729-37. doi: 10.1007/s00280-014-2554-1. Epub 2014 Aug 7. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- 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
- Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [Article]
- Brandon EF, Meijerman I, Klijn JS, den Arend D, Sparidans RW, Lazaro LL, Beijnen JH, Schellens JH: In-vitro cytotoxicity of ET-743 (Trabectedin, Yondelis), a marine anti-cancer drug, in the Hep G2 cell line: influence of cytochrome P450 and phase II inhibition, and cytochrome P450 induction. Anticancer Drugs. 2005 Oct;16(9):935-43. [Article]
- Lee JK, Leslie EM, Zamek-Gliszczynski MJ, Brouwer KL: Modulation of trabectedin (ET-743) hepatobiliary disposition by multidrug resistance-associated proteins (Mrps) may prevent hepatotoxicity. Toxicol Appl Pharmacol. 2008 Apr 1;228(1):17-23. doi: 10.1016/j.taap.2007.11.020. Epub 2007 Dec 3. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- 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
References
- Lee JK, Leslie EM, Zamek-Gliszczynski MJ, Brouwer KL: Modulation of trabectedin (ET-743) hepatobiliary disposition by multidrug resistance-associated proteins (Mrps) may prevent hepatotoxicity. Toxicol Appl Pharmacol. 2008 Apr 1;228(1):17-23. doi: 10.1016/j.taap.2007.11.020. Epub 2007 Dec 3. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
- Gene Name
- CYP2E1
- Uniprot ID
- P05181
- Uniprot Name
- Cytochrome P450 2E1
- Molecular Weight
- 56848.42 Da
References
- Lee JK, Leslie EM, Zamek-Gliszczynski MJ, Brouwer KL: Modulation of trabectedin (ET-743) hepatobiliary disposition by multidrug resistance-associated proteins (Mrps) may prevent hepatotoxicity. Toxicol Appl Pharmacol. 2008 Apr 1;228(1):17-23. doi: 10.1016/j.taap.2007.11.020. Epub 2007 Dec 3. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- 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
- Lee JK, Leslie EM, Zamek-Gliszczynski MJ, Brouwer KL: Modulation of trabectedin (ET-743) hepatobiliary disposition by multidrug resistance-associated proteins (Mrps) may prevent hepatotoxicity. Toxicol Appl Pharmacol. 2008 Apr 1;228(1):17-23. doi: 10.1016/j.taap.2007.11.020. Epub 2007 Dec 3. [Article]
Drug created at October 21, 2007 22:23 / Updated at February 20, 2024 23:54