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Identification
NameBortezomib
Accession NumberDB00188  (APRD00828)
Typesmall molecule
Groupsapproved, investigational
Description

Bortezomib (originally PS-341 and marketed as Velcade by Millennium Pharmaceuticals) is the first therapeutic proteasome inhibitor to be tested in humans. It is approved in the U.S. for treating relapsed multiple myeloma and mantle cell lymphoma. In multiple myeloma, complete clinical responses have been obtained in patients with otherwise refractory or rapidly advancing disease.

Structure
Thumb
SynonymsNot Available
SaltsNot Available
Brand names
NameCompany
VelcadeNot Available
Brand mixturesNot Available
CategoriesNot Available
CAS number179324-69-7
WeightAverage: 384.237
Monoisotopic: 384.196885774
Chemical FormulaC19H25BN4O4
InChI KeyInChIKey=GXJABQQUPOEUTA-RDJZCZTQSA-N
InChI
InChI=1S/C19H25BN4O4/c1-13(2)10-17(20(27)28)24-18(25)15(11-14-6-4-3-5-7-14)23-19(26)16-12-21-8-9-22-16/h3-9,12-13,15,17,27-28H,10-11H2,1-2H3,(H,23,26)(H,24,25)/t15-,17-/m0/s1
IUPAC Name
[(1R)-3-methyl-1-[(2S)-3-phenyl-2-(pyrazin-2-ylformamido)propanamido]butyl]boronic acid
SMILES
CC(C)C[C@H](NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)C1=CN=CC=N1)B(O)O
Mass SpecNot Available
Taxonomy
KingdomOrganic Compounds
SuperclassOrganic Acids and Derivatives
ClassCarboxylic Acids and Derivatives
SubclassAmino Acids, Peptides, and Analogues
Direct parentN-acyl-alpha Amino Acids and Derivatives
Alternative parentsAlpha Amino Acid Amides; Amphetamines and Derivatives; Phenylpropylamines; Pyrazinecarboxamides; Boronic Acids; Secondary Carboxylic Acid Amides; Carboxylic Acids; Polyamines; Enolates; Organoboron Compounds
Substituentsamphetamine or derivative; phenylpropylamine; pyrazinecarboxamide; pyrazine carboxylic acid or derivative; pyrazine; benzene; boronic acid; secondary carboxylic acid amide; carboxamide group; boronic acid derivative; polyamine; enolate; carboxylic acid; amine; organonitrogen compound; organic metalloid moeity; organoboron compound
Classification descriptionThis compound belongs to the n-acyl-alpha amino acids and derivatives. These are compounds containing an alpha amino acid (or a derivative thereof) which bears an acyl group at his terminal nitrogen atom.
Pharmacology
IndicationFor treatment of multiple myeloma in patients who have not been successfully treated with at least two previous therapies.
PharmacodynamicsBortezomib is a drug that inhibits the mammalian 26S proteasome. The ubiquitin-proteasome pathway plays an essential role in regulating the intracellular concentration of specific proteins, thereby maintaining homeostasis within cells. Inhibition of the 26S proteasome prevents this targeted proteolysis, which can affect multiple signaling cascades within the cell. This disruption of normal homeostatic mechanisms can lead to cell death. Experiments have demonstrated that bortezomib is cytotoxic to a variety of cancer cell types in vitro. Bortezomib causes a delay in tumor growth in vivo in nonclinical tumor models, including multiple myeloma. Tumor cells, that is, rapidly dividing cells, appear to be more sensitive to proteasome inhibition.
Mechanism of actionBortezomib is a reversible inhibitor of the chymotrypsin-like activity of the 26S proteasome in mammalian cells. The 26S proteasome is a large protein complex that degrades ubiquitinated proteins. The active site of the proteasome has chymotrypsin-like, trypsin-like, and postglutamyl peptide hydrolysis activity. The 26S proteasome degrades various proteins critical to cancer cell survival, such as cyclins, tumor suppressors, BCL-2, and cyclin-dependent kinase inhibitors. Inhibition of these degradations sensitizes cells to apoptosis. Bortezomib is a potent inhibitor of 26S proteasome, which sensitizes activity in dividing multiple myeloma and leukemic cells, thus inducing apoptosis. In addition, bortezomib appears to increase the sensitivity of cancer cells to traditional anticancer agents (e.g., gemcitabine, cisplatin, paclitaxel, irinotecan, and radiation).
AbsorptionNot Available
Volume of distributionNot Available
Protein binding83% over the concentration range of 100-1000 ng/ml.
Metabolism

In vitro studies with human liver microsomes and human cDNA-expressed cytochrome P450 isozymes indicate that bortezomib is primarily oxidatively metabolized via cytochrome P450 enzymes 3A4, 2C19, and 1A2, while bortezomib metabolism by CYP 2D6 and 2C9 enzymes is minor. The major metabolic pathway is deboronation to form 2 deboronated metabolites that subsequently undergo hydroxylation to several metabolites which are inactive as 26S proteasome inhibitors.

SubstrateEnzymesProduct
Bortezomib
Bortezomib metabolite M1Details
Bortezomib
Bortezomib metabolite M2Details
Bortezomib metabolite M1
    Bortezomib metabolite M3Details
    Bortezomib metabolite M2
      Bortezomib metabolite M3Details
      Bortezomib metabolite M3
        Bortezomib metabolite M4Details
        Bortezomib metabolite M1
          Bortezomib metabolite M5Details
          Bortezomib metabolite M2
            Bortezomib metabolite M6Details
            Bortezomib metabolite M2
            Bortezomib metabolite M8Details
            Bortezomib metabolite M8
              Bortezomib metabolite M33Details
              Bortezomib
                Bortezomib metabolite M34Details
                Bortezomib metabolite M1
                  Bortezomib metabolite M25Details
                  Bortezomib metabolite M1
                    Bortezomib metabolite M26Details
                    Bortezomib metabolite M2
                      Bortezomib metabolite M27Details
                      Bortezomib metabolite M2
                        Bortezomib metabolite M28Details
                        Bortezomib
                        Bortezomib metabolite M23 or M24 (1)Details
                        Bortezomib
                        Bortezomib metabolite M23 or M24 (2)Details
                        Route of eliminationThe pathways of elimination of bortezomib have not been characterized in humans.
                        Half lifeThe mean elimination half-life of bortezomib after first dose ranged from 9 to 15 hours at doses ranging from 1.45 to 2.00 mg/m2 in patients with advanced malignancies.
                        Clearance
                        • 102 L/h [patients with multiple myeloma following the first dose for doses of 1 mg/m2]
                        • 112 L/h [patients with multiple myeloma following the first dose for doses of 1.3 mg/m2]
                        • 15 – 32 L/h [patients with multiple myeloma following subsequent doses for doses of 1 and 1.3 mg/m2]
                        ToxicityCardiovascular safety pharmacology studies in monkeys show that lethal IV doses are associated with decreases in blood pressure, increases in heart rate, increases in contractility, and ultimately terminal hypotension. In monkeys, doses of 3.0 mg/m2 and greater (approximately twice the recommended clinical dose) resulted in progressive hypotension starting at 1 hour and progressing to death by 12 to 14 hours following drug administration.
                        Affected organisms
                        • Humans and other mammals
                        PathwaysNot Available
                        SNP Mediated EffectsNot Available
                        SNP Mediated Adverse Drug ReactionsNot Available
                        ADMET
                        Predicted ADMET features
                        Property Value Probability
                        Human Intestinal Absorption - 0.6935
                        Blood Brain Barrier - 0.6533
                        Caco-2 permeable - 0.6576
                        P-glycoprotein substrate Substrate 0.5909
                        P-glycoprotein inhibitor I Non-inhibitor 0.785
                        P-glycoprotein inhibitor II Non-inhibitor 1.0
                        Renal organic cation transporter Non-inhibitor 0.9445
                        CYP450 2C9 substrate Non-substrate 0.7145
                        CYP450 2D6 substrate Substrate 0.8918
                        CYP450 3A4 substrate Non-substrate 0.5209
                        CYP450 1A2 substrate Non-inhibitor 0.855
                        CYP450 2C9 substrate Non-inhibitor 0.8267
                        CYP450 2D6 substrate Non-inhibitor 0.9304
                        CYP450 2C19 substrate Non-inhibitor 0.8108
                        CYP450 3A4 substrate Non-inhibitor 0.7308
                        CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9604
                        Ames test Non AMES toxic 0.7439
                        Carcinogenicity Non-carcinogens 0.8064
                        Biodegradation Not ready biodegradable 0.9943
                        Rat acute toxicity 2.4537 LD50, mol/kg Not applicable
                        hERG inhibition (predictor I) Weak inhibitor 0.9936
                        hERG inhibition (predictor II) Non-inhibitor 0.8593
                        Pharmacoeconomics
                        Manufacturers
                        • Millennium pharmaceuticals inc
                        Packagers
                        Dosage forms
                        FormRouteStrength
                        Powder, for solutionIntravenous
                        Prices
                        Unit descriptionCostUnit
                        Velcade 3.5 mg vial1590.0USDvial
                        DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
                        Patents
                        CountryPatent NumberApprovedExpires (estimated)
                        United States67134462002-01-252022-01-25
                        United States60839031994-10-282014-10-28
                        Canada22039362005-04-122015-10-27
                        Properties
                        Statesolid
                        Experimental Properties
                        PropertyValueSource
                        water solubilityThe solubility of bortezomib, as the monomeric boronic acid, is 3.3 to 3.8 mg/mL in a pH range of 2 to 6.5.Not Available
                        Predicted Properties
                        PropertyValueSource
                        water solubility5.32e-02 g/lALOGPS
                        logP0.89ALOGPS
                        logP1.53ChemAxon
                        logS-3.9ALOGPS
                        pKa (strongest acidic)13.04ChemAxon
                        pKa (strongest basic)-0.7ChemAxon
                        physiological charge0ChemAxon
                        hydrogen acceptor count6ChemAxon
                        hydrogen donor count4ChemAxon
                        polar surface area124.44ChemAxon
                        rotatable bond count9ChemAxon
                        refractivity99.37ChemAxon
                        polarizability40.48ChemAxon
                        number of rings2ChemAxon
                        bioavailability1ChemAxon
                        rule of fiveYesChemAxon
                        Ghose filterYesChemAxon
                        Veber's ruleNoChemAxon
                        MDDR-like ruleNoChemAxon
                        Spectra
                        SpectraNot Available
                        References
                        Synthesis Reference

                        Raghavendracharyulu Venkata Palle, Rajasekhar Kadaboina, Veerendeer Murki, Amarendhar Manda, Nageshwar Gunda, Ramaseshagiri Rao Pulla, Mallesha Hanmanthu, Narasimha Naidu Mopidevi, Suresh Kumar Ramdoss, “BORTEZOMIB AND PROCESS FOR PRODUCING SAME.” U.S. Patent US20100226597, issued September 09, 2010.

                        US20100226597
                        General Reference
                        1. Adams J, Kauffman M: Development of the proteasome inhibitor Velcade (Bortezomib). Cancer Invest. 2004;22(2):304-11. Pubmed
                        2. Bonvini P, Zorzi E, Basso G, Rosolen A: Bortezomib-mediated 26S proteasome inhibition causes cell-cycle arrest and induces apoptosis in CD-30+ anaplastic large cell lymphoma. Leukemia. 2007 Apr;21(4):838-42. Epub 2007 Feb 1. Pubmed
                        3. Voorhees PM, Dees EC, O’Neil B, Orlowski RZ: The proteasome as a target for cancer therapy. Clin Cancer Res. 2003 Dec 15;9(17):6316-25. Pubmed
                        4. Oakervee HE, Popat R, Curry N, Smith P, Morris C, Drake M, Agrawal S, Stec J, Schenkein D, Esseltine DL, Cavenagh JD: PAD combination therapy (PS-341/bortezomib, doxorubicin and dexamethasone) for previously untreated patients with multiple myeloma. Br J Haematol. 2005 Jun;129(6):755-62. Pubmed
                        External Links
                        ResourceLink
                        ChEBI52717
                        ChEMBLCHEMBL325041
                        Therapeutic Targets DatabaseDAP001318
                        PharmGKBPA10252
                        Drug Product Database2262452
                        RxListhttp://www.rxlist.com/cgi/generic3/velcade.htm
                        Drugs.comhttp://www.drugs.com/cdi/bortezomib.html
                        WikipediaBortezomib
                        ATC CodesL01XX32
                        AHFS Codes
                        • 10:00.00
                        PDB EntriesNot Available
                        FDA labelshow(199 KB)
                        MSDSNot Available
                        Interactions
                        Drug Interactions
                        Drug
                        ClopidogrelModerate CYP2C19 Inhibitors like bortezomib may decrease serum concentrations of the active metabolite(s) of Clopidogrel. Avoid concurrent use of moderate CYP2C19 inhibitors with clopidogrel whenever possible. If such a combination must be used, monitor closely for evidence of reduced clinical response to clopidogrel.
                        EtravirineBortezombib, when used concomitantly with etravirine, may experience a decrease in serum concentration. It is recommended to avoid this combination.
                        TelithromycinTelithromycin may reduce clearance of Bortezomib. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Bortezomib if Telithromycin is initiated, discontinued or dose changed.
                        TiclopidineTiclopidine may decrease the metabolism and clearance of Bortezomib. Consider alternate therapy or monitor for adverse/toxic effects of Bortezomib if Ticlopidine is initiated, discontinued or dose changed.
                        VoriconazoleVoriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of bortezomib by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of bortezomib if voriconazole is initiated, discontinued or dose changed.
                        Food Interactions
                        • Citrus fruits - Patients should avoid taking extra vitamin C (ascorbic acid) supplements and vitamin C-containing multi-vitamins during their bortezomib therapy. Ascorbic Acid may diminish the therapeutic effect of Bortezomib.
                        • Green Tea - Green Tea may diminish the antineoplastic effect of Bortezomib. Avoid concurrent use of green tea extract and other green tea products during treatment with bortezomib.

                        1. 26S proteasome non-ATPase regulatory subunit 2

                        Kind: protein

                        Organism: Human

                        Pharmacological action: yes

                        Actions: inhibitor

                        Components

                        Name UniProt ID Details
                        26S proteasome non-ATPase regulatory subunit 2 Q13200 Details

                        References:

                        1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
                        2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed
                        3. von Schwarzenberg K, Held SA, Schaub A, Brauer KM, Bringmann A, Brossart P: Proteasome inhibition overcomes the resistance of renal cell carcinoma cells against the PPARgamma ligand troglitazone. Cell Mol Life Sci. 2009 Apr;66(7):1295-308. Pubmed
                        4. Marchi E, Paoluzzi L, Scotto L, Seshan VE, Zain JM, Zinzani PL, O’Connor OA: Pralatrexate is synergistic with the proteasome inhibitor bortezomib in in vitro and in vivo models of T-cell lymphoid malignancies. Clin Cancer Res. 2010 Jul 15;16(14):3648-58. Epub 2010 May 25. Pubmed
                        5. Saeki Y, Fukunaga K, Tanaka K: [Proteasome inhibitors]. Nippon Rinsho. 2010 Oct;68(10):1818-22. Pubmed

                        2. Proteasome subunit beta type-1

                        Kind: protein

                        Organism: Human

                        Pharmacological action: yes

                        Actions: antagonist

                        Components

                        Name UniProt ID Details
                        Proteasome subunit beta type-1 P20618 Details

                        References:

                        1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
                        2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed
                        3. Saeki Y, Fukunaga K, Tanaka K: [Proteasome inhibitors]. Nippon Rinsho. 2010 Oct;68(10):1818-22. Pubmed

                        3. Proteasome subunit beta type-5

                        Kind: protein

                        Organism: Human

                        Pharmacological action: yes

                        Actions: antagonist

                        Components

                        Name UniProt ID Details
                        Proteasome subunit beta type-5 P28074 Details

                        References:

                        1. Politou M, Karadimitris A, Terpos E, Kotsianidis I, Apperley JF, Rahemtulla A: No evidence of mutations of the PSMB5 (beta-5 subunit of proteasome) in a case of myeloma with clinical resistance to Bortezomib. Leuk Res. 2006 Feb;30(2):240-1. Epub 2005 Aug 2. Pubmed
                        2. Saeki Y, Fukunaga K, Tanaka K: [Proteasome inhibitors]. Nippon Rinsho. 2010 Oct;68(10):1818-22. Pubmed

                        4. Proteasome subunit beta type-2

                        Kind: protein

                        Organism: Human

                        Pharmacological action: yes

                        Actions: antagonist

                        Components

                        Name UniProt ID Details
                        Proteasome subunit beta type-2 P49721 Details

                        References:

                        1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
                        2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed
                        3. Saeki Y, Fukunaga K, Tanaka K: [Proteasome inhibitors]. Nippon Rinsho. 2010 Oct;68(10):1818-22. Pubmed

                        5. 26S proteasome non-ATPase regulatory subunit 1

                        Kind: protein

                        Organism: Human

                        Pharmacological action: yes

                        Actions: inhibitor

                        Components

                        Name UniProt ID Details
                        26S proteasome non-ATPase regulatory subunit 1 Q99460 Details

                        References:

                        1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
                        2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed
                        3. Saeki Y, Fukunaga K, Tanaka K: [Proteasome inhibitors]. Nippon Rinsho. 2010 Oct;68(10):1818-22. Pubmed

                        1. Cytochrome P450 3A4

                        Kind: protein

                        Organism: Human

                        Pharmacological action: unknown

                        Actions: substrate inhibitor

                        Components

                        Name UniProt ID Details
                        Cytochrome P450 3A4 P08684 Details

                        References:

                        1. 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. Pubmed
                        2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
                        3. Lexicomp.

                        2. Cytochrome P450 2C19

                        Kind: protein

                        Organism: Human

                        Pharmacological action: unknown

                        Actions: substrate inhibitor

                        Components

                        Name UniProt ID Details
                        Cytochrome P450 2C19 P33261 Details

                        References:

                        1. 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. Pubmed
                        2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
                        3. Lexicomp

                        3. Cytochrome P450 2D6

                        Kind: protein

                        Organism: Human

                        Pharmacological action: unknown

                        Actions: substrate inhibitor

                        Components

                        Name UniProt ID Details
                        Cytochrome P450 2D6 P10635 Details

                        References:

                        1. 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. Pubmed
                        2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
                        3. Lexicomp.

                        4. Cytochrome P450 1A2

                        Kind: protein

                        Organism: Human

                        Pharmacological action: unknown

                        Actions: substrate inhibitor

                        Components

                        Name UniProt ID Details
                        Cytochrome P450 1A2 P05177 Details

                        References:

                        1. 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. Pubmed
                        2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
                        3. Lexicomp.

                        5. Cytochrome P450 2C9

                        Kind: protein

                        Organism: Human

                        Pharmacological action: unknown

                        Actions: substrate inhibitor

                        Components

                        Name UniProt ID Details
                        Cytochrome P450 2C9 P11712 Details

                        References:

                        1. 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. Pubmed
                        2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

                        6. Prostaglandin G/H synthase 1

                        Kind: protein

                        Organism: Human

                        Pharmacological action: unknown

                        Actions: substrate

                        Components

                        Name UniProt ID Details
                        Prostaglandin G/H synthase 1 P23219 Details

                        References:

                        1. 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. Pubmed

                        7. Cytochrome P450 1A1

                        Kind: protein

                        Organism: Human

                        Pharmacological action: unknown

                        Actions: inhibitor

                        Components

                        Name UniProt ID Details
                        Cytochrome P450 1A1 P04798 Details

                        References:

                        1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

                        8. Cytochrome P450 2C8

                        Kind: protein

                        Organism: Human

                        Pharmacological action: unknown

                        Actions: inhibitor

                        Components

                        Name UniProt ID Details
                        Cytochrome P450 2C8 P10632 Details

                        References:

                        1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

                        1. High affinity copper uptake protein 1

                        Kind: protein

                        Organism: Human

                        Pharmacological action: unknown

                        Actions: inhibitor

                        Components

                        Name UniProt ID Details
                        High affinity copper uptake protein 1 O15431 Details

                        References:

                        1. Jandial DD, Farshchi-Heydari S, Larson CA, Elliott GI, Wrasidlo WJ, Howell SB: Enhanced delivery of cisplatin to intraperitoneal ovarian carcinomas mediated by the effects of bortezomib on the human copper transporter 1. Clin Cancer Res. 2009 Jan 15;15(2):553-60. Pubmed

                        Comments
                        Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:08