Identification

Name
Carboplatin
Accession Number
DB00958
Description

An organoplatinum compound that possesses antineoplastic activity.

Type
Small Molecule
Groups
Approved
Structure
Thumb
Weight
Average: 371.254
Monoisotopic: 371.044481331
Chemical Formula
C6H12N2O4Pt
Synonyms
  • Carboplatin
  • Carboplatine
  • Carboplatino
  • CBDCA
  • cis-(1,1-cyclobutanedicarboxylato)diammineplatinum(II)
  • cis-diammine(1,1-cyclobutanedicarboxylato)platinum
  • cis-diammine(1,1-cyclobutanedicarboxylato)platinum(II)
External IDs
  • NSC-241240

Pharmacology

Indication

For the initial treatment of advanced ovarian carcinoma in established combination with other approved chemotherapeutic agents. One established combination regimen consists of PARAPLATIN and cyclophosphamide. It is also indicated for the palliative treatment of patients with ovarian carcinoma recurrent after prior chemotherapy, including patients who have been previously treated with cisplatin.

Associated Conditions
Associated Therapies
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
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Pharmacodynamics

Carboplatin is an antineoplastic in the class of alkylating agents and is used to treat various forms of cancer. Alkylating agents are so named because of their ability to add alkyl groups to many electronegative groups under conditions present in cells. They stop tumor growth by cross-linking guanine bases in DNA double-helix strands - directly attacking DNA. This makes the strands unable to uncoil and separate. As this is necessary in DNA replication, the cells can no longer divide. In addition, these drugs add methyl or other alkyl groups onto molecules where they do not belong which in turn inhibits their correct utilization by base pairing and causes a miscoding of DNA. Alkylating agents are cell cycle-nonspecific. Alkylating agents work by three different mechanisms all of which achieve the same end result - disruption of DNA function and cell death.

Mechanism of action

Alkylating agents work by three different mechanisms: 1) attachment of alkyl groups to DNA bases, resulting in the DNA being fragmented by repair enzymes in their attempts to replace the alkylated bases, preventing DNA synthesis and RNA transcription from the affected DNA, 2) DNA damage via the formation of cross-links (bonds between atoms in the DNA) which prevents DNA from being separated for synthesis or transcription, and 3) the induction of mispairing of the nucleotides leading to mutations.

TargetActionsOrganism
ADNA
cross-linking/alkylation
Humans
Absorption

The Cmax values and areas under the plasma concentration versus time curves from 0 to infinity (AUC inf) increase linearly with dose, although the increase was slightly more than dose proportional. Carboplatin exhibits linear pharmacokinetics.

Volume of distribution
  • 16 L [apparent volume of distribution, 30 minute IV infusion of 300 mg/m^2 to 500 mg/m^2]
Protein binding

Carboplatin is not bound to plasma protein. However, the platinum itself from carboplatin irreversibly binds to plasma proteins and is slowly eliminated with a minimum half-life of 5 days.

Metabolism
Not Available
Route of elimination

The major route of elimination of carboplatin is renal excretion. After 24 hours, all of the platinum is recovered in the urine as carboplatin. Whether biliary excretion occurs is not known.

Half-life

Initial plasma half-life (alpha) = 1.1 to 2 hours; Post distribution plasma half-life (beta) = 2.6 - 5.9 hours.

Clearance
  • 4.4 L/hour [total body clearance, 30 minute IV infusion of 300 mg/m^2 to 500 mg/m^2]
Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More
Toxicity

Toxic by ingestion. May be create toxic effect through inhalation or skin contact. May cause reproductive defects. May act as a sensitizer. ORL-RAT LD50 343 mg kg-1; SCN-RAT LD50 72 mg kg-1; IPN-MUS LD50 118 mg kg-1

Affected organisms
  • Humans and other mammals
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.
DrugInteraction
AbacavirCarboplatin may decrease the excretion rate of Abacavir which could result in a higher serum level.
AbataceptThe risk or severity of adverse effects can be increased when Carboplatin is combined with Abatacept.
AbciximabThe risk or severity of bleeding can be increased when Abciximab is combined with Carboplatin.
AcarboseCarboplatin may decrease the excretion rate of Acarbose which could result in a higher serum level.
AceclofenacCarboplatin may decrease the excretion rate of Aceclofenac which could result in a higher serum level.
AcemetacinAcemetacin may decrease the excretion rate of Carboplatin which could result in a higher serum level.
AcenocoumarolThe risk or severity of bleeding can be increased when Carboplatin is combined with Acenocoumarol.
AcetaminophenCarboplatin may decrease the excretion rate of Acetaminophen which could result in a higher serum level.
AcetazolamideAcetazolamide may increase the excretion rate of Carboplatin which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acidAcetylsalicylic acid may decrease the excretion rate of Carboplatin which could result in a higher serum level.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
  • Avoid echinacea. Co-administration may decrease effectiveness of immunosuppressants.

Products

International/Other Brands
Paraplatin-AQ
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Carboplatin InjectionLiquidIntravenousTEVA Canada Limited1994-12-31Not applicableCanada flag
Carboplatin InjectionSolutionIntravenousOmega Laboratories Ltd2013-06-10Not applicableCanada flag
Carboplatin Injection BPSolutionIntravenousAccord Healthcare Inc2015-03-11Not applicableCanada flag
Carboplatin Injection BPSolutionIntravenousPfizer Canada Ulc1997-07-30Not applicableCanada flag
Carboplatin Injection Liq 10mg/mlLiquidIntravenousDavid Bull Laboratories (Pty) Ltd.1992-12-311998-08-13Canada flag
Carboplatin Injection, BPSolutionIntravenousStrides Pharma Canada IncNot applicableNot applicableCanada flag
ParaplatinInjection, solution10 mg/1mLIntravenousE.R. Squibb & Sons, L.L.C.2007-01-012008-06-30US flag
ParaplatinInjection, powder, lyophilized, for solution450 mg/45mLIntravenousE.R. Squibb & Sons, L.L.C.2008-01-012009-04-14US flag
ParaplatinInjection, solution10 mg/1mLIntravenousE.R. Squibb & Sons, L.L.C.2006-01-012007-12-31US flag
ParaplatinInjection, solution10 mg/1mLIntravenousE.R. Squibb & Sons, L.L.C.2007-01-012008-09-30US flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
CarboplatinInjection, solution10 mg/1mLIntravenousMeitheal Pharmaceuticals Inc.2017-06-19Not applicableUS flag
CarboplatinInjection, solution10 mg/1mLIntravenousGland Pharma Limited2017-02-20Not applicableUS flag
CarboplatinInjection, solution10 mg/1mLIntravenousAlvogen Inc.2018-02-012019-09-01US flag
CarboplatinInjection, solution150 mg/15mLIntravenousIngenus Pharmaceuticals, LLC2017-05-06Not applicableUS flag
CarboplatinInjection, powder, lyophilized, for solution150 mg/15mLIntravenousPliva, Inc.2009-10-152010-10-31US flag
CarboplatinInjection10 mg/1mLIntravenousBedford Pharmaceuticals2004-10-142010-06-30US flag
CarboplatinInjection10 mg/1mLIntravenousMylan Institutional2011-11-092017-12-31US flag
CarboplatinInjection10 mg/1mLIntravenousSun Pharmaceutical Industries, Inc.2008-09-192016-06-30US flag
CarboplatinInjection, solution10 mg/1mLIntravenousSun Pharma Global Inc.2008-09-192014-06-27US flag
CarboplatinInjection, solution150 mg/15mLIntravenousCipla USA Inc.2007-01-18Not applicableUS flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more

Categories

ATC Codes
L01XA02 — Carboplatin
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as dicarboxylic acids and derivatives. These are organic compounds containing exactly two carboxylic acid groups.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
Carboxylic acids and derivatives
Sub Class
Dicarboxylic acids and derivatives
Direct Parent
Dicarboxylic acids and derivatives
Alternative Parents
Carboxylic acid salts / Oxacyclic compounds / Organic transition metal salts / Metalloheterocyclic compounds / Organic oxides / Organic nitrogen compounds / Hydrocarbon derivatives / Carbonyl compounds
Substituents
Aliphatic heteropolycyclic compound / Carbonyl group / Carboxylic acid salt / Dicarboxylic acid or derivatives / Hydrocarbon derivative / Metalloheterocycle / Organic metal salt / Organic nitrogen compound / Organic oxide / Organic oxygen compound
Molecular Framework
Aliphatic heteropolycyclic compounds
External Descriptors
platinum coordination entity (CHEBI:31355)

Chemical Identifiers

UNII
BG3F62OND5
CAS number
41575-94-4
InChI Key
OLESAACUTLOWQZ-UHFFFAOYSA-L
InChI
InChI=1S/C6H8O4.2H3N.Pt/c7-4(8)6(5(9)10)2-1-3-6;;;/h1-3H2,(H,7,8)(H,9,10);2*1H3;/q;;;+2/p-2
IUPAC Name
7,7-diamino-6,8-dioxa-7-platinaspiro[3.5]nonane-5,9-dione
SMILES
[H][N]([H])([H])[Pt]1(OC(=O)C2(CCC2)C(=O)O1)[N]([H])([H])[H]

References

Synthesis Reference

Jingzun Wang, Huisheng Qu, Lei Wang, Ting Wang, "Supermolecular carboplatin derivatives, their preparation and pharmaceutical composition containing them as active ingredient and applications of the compositions." U.S. Patent US07259270, issued August 21, 2007.

US07259270
General References
  1. Natarajan G, Malathi R, Holler E: Increased DNA-binding activity of cis-1,1-cyclobutanedicarboxylatodiammineplatinum(II) (carboplatin) in the presence of nucleophiles and human breast cancer MCF-7 cell cytoplasmic extracts: activation theory revisited. Biochem Pharmacol. 1999 Nov 15;58(10):1625-9. [PubMed:10535754]
  2. Knox RJ, Friedlos F, Lydall DA, Roberts JJ: Mechanism of cytotoxicity of anticancer platinum drugs: evidence that cis-diamminedichloroplatinum(II) and cis-diammine-(1,1-cyclobutanedicarboxylato)platinum(II) differ only in the kinetics of their interaction with DNA. Cancer Res. 1986 Apr;46(4 Pt 2):1972-9. [PubMed:3512077]
  3. Canetta R, Rozencweig M, Carter SK: Carboplatin: the clinical spectrum to date. Cancer Treat Rev. 1985 Sep;12 Suppl A:125-36. [PubMed:3002623]
Human Metabolome Database
HMDB0015093
KEGG Drug
D01363
PubChem Compound
38904
PubChem Substance
46507170
ChemSpider
8514637
RxNav
40048
ChEBI
31355
ChEMBL
CHEMBL1351
Therapeutic Targets Database
DAP000535
PharmGKB
PA448803
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Carboplatin
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
FDA label
Download (1.26 MB)
MSDS
Download (73.5 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentBreast Cancer1
4CompletedTreatmentAdenocarcinomas / Carcinoma NOS / Carcinoma, Large Cell / Neoplasms, Lung / Non-Small Cell Lung Carcinoma (NSCLC) / Squamous Cell Carcinoma (SCC)1
4CompletedTreatmentCarcinoma, Large Cell / Neuroendocrine Tumors1
4CompletedTreatmentNon-Small Cell Lung Carcinoma (NSCLC)3
4CompletedTreatmentRetinoblastoma1
4Not Yet RecruitingTreatmentBreast Cancer1
4Not Yet RecruitingTreatmentNon-Small Cell Lung Carcinoma (NSCLC)1
4RecruitingTreatmentCentral Nervous System Embryonal Tumors / Medulloblastomas1
4RecruitingTreatmentEfficacy and Safety1
4RecruitingTreatmentSquamous Cell Carcinoma of the Head and Neck (SCCHN)1

Pharmacoeconomics

Manufacturers
  • App pharmaceuticals llc
  • Bedford laboratories div ben venue laboratories inc
  • Hospira inc
  • Pliva inc
  • Sandoz inc
  • Watson laboratories inc
  • Watson laboratories
  • Bristol myers squibb co pharmaceutical research institute
  • Akorn inc
  • Bedford laboratories
  • Bioniche pharma usa llc
  • Ebewe pharma ges mbh nfg kg
  • Fresenius kabi oncology plc
  • Pharmachemie bv
  • Pliva lachema as
  • Spectrum pharmaceuticals inc
  • Sun pharma global inc
  • Teva parenteral medicines inc
  • Bristol myers squibb co
Packagers
  • APP Pharmaceuticals
  • Baxter International Inc.
  • Bedford Labs
  • Bell-More Laboratories Inc.
  • Ben Venue Laboratories Inc.
  • Bristol-Myers Squibb Co.
  • Cipla Ltd.
  • Ebewe Pharma
  • Fresenius Kabi AB
  • Generamedix Inc.
  • Hospira Inc.
  • Intas Pharmaceuticals Ltd.
  • Mead Johnson and Co.
  • Otn Generics Inc.
  • Pharmachemie BV
  • Pliva Inc.
  • Spectrum Pharmaceuticals
  • Teva Pharmaceutical Industries Ltd.
  • Watson Pharmaceuticals
Dosage Forms
FormRouteStrength
Injection, powder, lyophilized, for solutionIntravenous150 mg
InjectionIntravenous1000 mg/100ml
InjectionIntravenous150 mg/15ml
InjectionIntravenous450 mg/45ml
InjectionIntravenous50 mg/5ml
InjectionIntravenous600 mg/60ml
Injection
InjectionIntravenous10 mg/1mL
Injection, powder, lyophilized, for solutionIntravenous10 mg/1mL
Injection, solutionIntravenous150 mg/15mL
Injection, solutionIntravenous450 mg/45mL
Injection, solutionIntravenous50 mg/5mL
Injection, solutionIntravenous600 mg/60mL
Injection, solution, concentrateIntravenous50 mg/5mL
SolutionIntravenous150 mg/5mL
SolutionIntravenous450 mg/5mL
SolutionIntravenous50 mg/5mL
Injection, solution, concentrateIntravenous10 mg/ml
Injection, solution, concentrateParenteral10 mg/ml
Injection, powder, for solutionIntravenous150 mg
LiquidIntravenous
SolutionIntravenous
SolutionIntravenous450 mg/45ml
SolutionIntravenous600 mg/60ml
Injection, solution, concentrateParenteral450 mg
SolutionIntravenous150 mg/15ml
Injection, solutionIntravenous1000 mg/100ml
Injection, powder, lyophilized, for solutionIntravenous450 mg
Injection, solution, concentrateIntravenous; Parenteral10 MG/ML
Injection, solutionParenteral150 MG/15ML
Injection, solutionParenteral450 MG/45ML
Injection, solutionParenteral50 MG/5ML
Injection, solutionIntravenous; Parenteral150 MG/15ML
Injection, solutionIntravenous; Parenteral450 MG/45ML
Injection, solutionIntravenous; Parenteral50 MG/5ML
Injection, solutionIntravenous; Parenteral600 MG/60ML
Injection, solution, concentrateIntravenous600 mg
SolutionIntravenous150 mg
InjectionIntravenous
Injection, solution, concentrateIntravenous600 mg/60mL
SolutionIntravenous450 mg
Injection, solution, concentrateIntravenous150 mg/15mL
Injection, solution, concentrateIntravenous450 mg/45mL
Injection, powder, for solutionIntravenous50 mg
Injection, powder, lyophilized, for solutionIntravenous150 mg/15mL
Injection, powder, lyophilized, for solutionIntravenous450 mg/45mL
Injection, powder, lyophilized, for solutionIntravenous50 mg/5mL
Injection, solutionIntravenous10 mg/1mL
Powder, for solutionIntravenous
Injection, solutionIntravenous150 mg
Injection, solutionIntravenous450 mg
Prices
Unit descriptionCostUnit
Paraplatin 450 mg vial1474.46USD vial
Paraplatin 150 mg vial491.48USD vial
Carboplatin 150 mg vial255.31USD vial
Paraplatin 50 mg vial163.84USD vial
Carboplatin 450 mg vial156.25USD vial
Carboplatin 50 mg vial85.1USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility79.8 mg/mLALOGPS
logP0.14ALOGPS
logS-0.67ALOGPS
Physiological Charge0ChemAxon
Hydrogen Acceptor Count0ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area107.88 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity60.04 m3·mol-1ChemAxon
Polarizability18.27 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption-0.6183
Blood Brain Barrier+0.8295
Caco-2 permeable-0.584
P-glycoprotein substrateNon-substrate0.6375
P-glycoprotein inhibitor INon-inhibitor0.9489
P-glycoprotein inhibitor IINon-inhibitor0.9968
Renal organic cation transporterNon-inhibitor0.9239
CYP450 2C9 substrateNon-substrate0.8745
CYP450 2D6 substrateNon-substrate0.8276
CYP450 3A4 substrateNon-substrate0.703
CYP450 1A2 substrateNon-inhibitor0.8142
CYP450 2C9 inhibitorNon-inhibitor0.854
CYP450 2D6 inhibitorNon-inhibitor0.9168
CYP450 2C19 inhibitorNon-inhibitor0.8607
CYP450 3A4 inhibitorNon-inhibitor0.6995
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9896
Ames testNon AMES toxic0.746
CarcinogenicityNon-carcinogens0.8906
BiodegradationReady biodegradable0.8235
Rat acute toxicity2.3469 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9596
hERG inhibition (predictor II)Non-inhibitor0.9767
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Kind
Nucleotide
Organism
Humans
Pharmacological action
Yes
Actions
Cross-linking/alkylation
DNA is the molecule of heredity, as it is responsible for the genetic propagation of most inherited traits. It is a polynucleic acid that carries genetic information on cell growth, division, and function. DNA consists of two long strands of nucleotides twisted into a double helix and held together by hydrogen bonds. The sequence of nucleotides determines hereditary characteristics. Each strand serves as the template for subsequent DNA replication and as a template for mRNA production, leading to protein synthesis via ribosomes.
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:17139284]
  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:17016423]
  3. Sharma S, Gong P, Temple B, Bhattacharyya D, Dokholyan NV, Chaney SG: Molecular dynamic simulations of cisplatin- and oxaliplatin-d(GG) intrastand cross-links reveal differences in their conformational dynamics. J Mol Biol. 2007 Nov 9;373(5):1123-40. Epub 2007 Aug 23. [PubMed:17900616]
  4. Appleton K, Mackay HJ, Judson I, Plumb JA, McCormick C, Strathdee G, Lee C, Barrett S, Reade S, Jadayel D, Tang A, Bellenger K, Mackay L, Setanoians A, Schatzlein A, Twelves C, Kaye SB, Brown R: Phase I and pharmacodynamic trial of the DNA methyltransferase inhibitor decitabine and carboplatin in solid tumors. J Clin Oncol. 2007 Oct 10;25(29):4603-9. [PubMed:17925555]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Xanthine oxidase activity
Specific Function
Key enzyme in purine degradation. Catalyzes the oxidation of hypoxanthine to xanthine. Catalyzes the oxidation of xanthine to uric acid. Contributes to the generation of reactive oxygen species. Ha...
Gene Name
XDH
Uniprot ID
P47989
Uniprot Name
Xanthine dehydrogenase/oxidase
Molecular Weight
146422.99 Da
References
  1. Husai K, Jagannathan R, Hasan Z, Trammell GL, Rybak LP, Hazelrigg SR, Somani SM: Dose response of carboplatin-induced nephrotoxicity in rats. Pharmacol Toxicol. 2002 Aug;91(2):83-9. [PubMed:12420797]
  2. Husain K, Whitworth C, Rybak LP: Time response of carboplatin-induced nephrotoxicity in rats. Pharmacol Res. 2004 Sep;50(3):291-300. [PubMed:15225673]
  3. Husain K, Whitworth C, Somani SM, Rybak LP: Carboplatin-induced oxidative stress in rat cochlea. Hear Res. 2001 Sep;159(1-2):14-22. [PubMed:11520631]
  4. Husain K, Whitworth C, Hazelrigg S, Rybak L: Carboplatin-induced oxidative injury in rat inferior colliculus. Int J Toxicol. 2003 Sep-Oct;22(5):335-42. [PubMed:14555405]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Peroxidase activity
Specific Function
Part of the host defense system of polymorphonuclear leukocytes. It is responsible for microbicidal activity against a wide range of organisms. In the stimulated PMN, MPO catalyzes the production o...
Gene Name
MPO
Uniprot ID
P05164
Uniprot Name
Myeloperoxidase
Molecular Weight
83867.71 Da
References
  1. Link [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Glutathione transferase activity
Specific Function
Conjugation of reduced glutathione to a wide number of exogenous and endogenous hydrophobic electrophiles. Acts on 1,2-epoxy-3-(4-nitrophenoxy)propane, phenethylisothiocyanate 4-nitrobenzyl chlorid...
Gene Name
GSTT1
Uniprot ID
P30711
Uniprot Name
Glutathione S-transferase theta-1
Molecular Weight
27334.755 Da
References
  1. Link [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Zinc ion binding
Specific Function
Metallothioneins have a high content of cysteine residues that bind various heavy metals; these proteins are transcriptionally regulated by both heavy metals and glucocorticoids.
Gene Name
MT1A
Uniprot ID
P04731
Uniprot Name
Metallothionein-1A
Molecular Weight
6120.19 Da
References
  1. Link [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Zinc ion binding
Specific Function
Metallothioneins have a high content of cysteine residues that bind various heavy metals; these proteins are transcriptionally regulated by both heavy metals and glucocorticoids.
Gene Name
MT2A
Uniprot ID
P02795
Uniprot Name
Metallothionein-2
Molecular Weight
6042.05 Da
References
  1. Link [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Zinc ion binding
Specific Function
Destroys radicals which are normally produced within the cells and which are toxic to biological systems.
Gene Name
SOD1
Uniprot ID
P00441
Uniprot Name
Superoxide dismutase [Cu-Zn]
Molecular Weight
15935.685 Da
References
  1. Husain K, Scott B, Whitworth C, Rybak LP: Time response of carboplatin-induced hearing loss in rat. Hear Res. 2004 May;191(1-2):110-8. doi: 10.1016/j.heares.2004.01.011. [PubMed:15109710]
  2. Husain K, Whitworth C, Somani SM, Rybak LP: Partial protection by lipoic acid against carboplantin-induced ototoxicity in rats. Biomed Environ Sci. 2005 Jun;18(3):198-206. [PubMed:16131024]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
S-nitrosoglutathione binding
Specific Function
Conjugation of reduced glutathione to a wide number of exogenous and endogenous hydrophobic electrophiles. Regulates negatively CDK5 activity via p25/p35 translocation to prevent neurodegeneration.
Gene Name
GSTP1
Uniprot ID
P09211
Uniprot Name
Glutathione S-transferase P
Molecular Weight
23355.625 Da
References
  1. Link [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Protein homodimerization activity
Specific Function
Conjugation of reduced glutathione to a wide number of exogenous and endogenous hydrophobic electrophiles.
Gene Name
GSTM1
Uniprot ID
P09488
Uniprot Name
Glutathione S-transferase Mu 1
Molecular Weight
25711.555 Da
References
  1. Link [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Superoxide dismutase activity
Specific Function
The enzyme apparently serves as a quinone reductase in connection with conjugation reactions of hydroquinons involved in detoxification pathways as well as in biosynthetic processes such as the vit...
Gene Name
NQO1
Uniprot ID
P15559
Uniprot Name
NAD(P)H dehydrogenase [quinone] 1
Molecular Weight
30867.405 Da
References
  1. Link [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Copper uptake transmembrane transporter activity
Specific Function
High-affinity, saturable copper transporter involved in dietary copper uptake.
Gene Name
SLC31A1
Uniprot ID
O15431
Uniprot Name
High affinity copper uptake protein 1
Molecular Weight
21090.545 Da
References
  1. Howell SB, Safaei R, Larson CA, Sailor MJ: Copper transporters and the cellular pharmacology of the platinum-containing cancer drugs. Mol Pharmacol. 2010 Jun;77(6):887-94. doi: 10.1124/mol.109.063172. Epub 2010 Feb 16. [PubMed:20159940]
  2. Song IS, Savaraj N, Siddik ZH, Liu P, Wei Y, Wu CJ, Kuo MT: Role of human copper transporter Ctr1 in the transport of platinum-based antitumor agents in cisplatin-sensitive and cisplatin-resistant cells. Mol Cancer Ther. 2004 Dec;3(12):1543-9. [PubMed:15634647]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Copper ion transmembrane transporter activity
Specific Function
Involved in low-affinity copper uptake.
Gene Name
SLC31A2
Uniprot ID
O15432
Uniprot Name
Probable low affinity copper uptake protein 2
Molecular Weight
15681.29 Da
References
  1. Blair BG, Larson CA, Safaei R, Howell SB: Copper transporter 2 regulates the cellular accumulation and cytotoxicity of Cisplatin and Carboplatin. Clin Cancer Res. 2009 Jul 1;15(13):4312-21. doi: 10.1158/1078-0432.CCR-09-0311. Epub 2009 Jun 9. [PubMed:19509135]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Superoxide dismutase copper chaperone activity
Specific Function
May supply copper to copper-requiring proteins within the secretory pathway, when localized in the trans-Golgi network. Under conditions of elevated extracellular copper, it relocalized to the plas...
Gene Name
ATP7A
Uniprot ID
Q04656
Uniprot Name
Copper-transporting ATPase 1
Molecular Weight
163372.275 Da
References
  1. Samimi G, Katano K, Holzer AK, Safaei R, Howell SB: Modulation of the cellular pharmacology of cisplatin and its analogs by the copper exporters ATP7A and ATP7B. Mol Pharmacol. 2004 Jul;66(1):25-32. [PubMed:15213293]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Copper-exporting atpase activity
Specific Function
Involved in the export of copper out of the cells, such as the efflux of hepatic copper into the bile.
Gene Name
ATP7B
Uniprot ID
P35670
Uniprot Name
Copper-transporting ATPase 2
Molecular Weight
157261.34 Da
References
  1. Samimi G, Katano K, Holzer AK, Safaei R, Howell SB: Modulation of the cellular pharmacology of cisplatin and its analogs by the copper exporters ATP7A and ATP7B. Mol Pharmacol. 2004 Jul;66(1):25-32. [PubMed:15213293]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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
References
  1. Ceckova M, Vackova Z, Radilova H, Libra A, Buncek M, Staud F: Effect of ABCG2 on cytotoxicity of platinum drugs: interference of EGFP. Toxicol In Vitro. 2008 Dec;22(8):1846-52. doi: 10.1016/j.tiv.2008.09.001. Epub 2008 Sep 9. [PubMed:18801423]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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
References
  1. Link [Link]

Drug created on June 13, 2005 07:24 / Updated on October 21, 2020 01:55

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