Identification
NameDacarbazine
Accession NumberDB00851  (APRD00331)
TypeSmall Molecule
GroupsApproved, Investigational
Description

An antineoplastic agent. It has significant activity against melanomas. (from Martindale, The Extra Pharmacopoeia, 31st ed, p564). Dacarbazine with Oblimersen is in clinical trials for the treatment of malignant melanoma.

Structure
Thumb
Synonyms
4-(3,3-dimethyl-1-triazeno)imidazole-5-carboxamide
4-(5)-(3,3-dimethyl-1-triazeno)imidazole-5(4)-carboxamide
4-(dimethyltriazeno)imidazole-5-carboxamide
5-(3,3-dimethyl-1-triazeno)imidazole-4-carboxamide
5-(3,3-dimethyltriazeno)imidazole-4-carboxamide
5-(dimethyltriazeno)imidazole-4-carboxamide
Biocarbazine
Dacarbazin
Dacarbazina
Dacarbazine
Dacarbazinum
DIC
DTCI
ICDMT
External IDs HSDB 3219 / NCI C04717 / NCI-C04717 / NSC 45 388 / NSC 45388 / NSC-45388
Product Ingredients Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Dacarbazine for Injection BPPowder, for solution600 mgIntravenousHospira, Inc.2000-04-04Not applicableCanada
Dtic Dome Inj 200mg/vialLiquid200 mgIntravenousMiles Inc. Pharmaceutical Division1976-12-311998-09-25Canada
Dtic-dome -pws IV 200mg/vialPowder, for solution10 mgIntravenousBayer1996-10-102005-05-31Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
DacarbazineInjection, powder, for solution200 mg/20mLIntravenousTeva Parenteral Medicines, Inc.1998-08-27Not applicableUs
DacarbazineInjection, powder, for solution10 mg/mLIntravenousHospira Worldwide, Inc.2001-10-18Not applicableUs
DacarbazineInjection, powder, for solution10 mg/mLIntravenousAPP Pharmaceuticals, Inc.2001-09-07Not applicableUs
DacarbazineInjection, powder, for solution10 mg/mLIntravenousAPP Pharmaceuticals, Inc.2001-09-07Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
DacaticOrion Corporation
DéticèneSanofi-Aventis
DeticeneSanofi-Aventis
Detimedacmedac GmbH
DTICBayer AG
DTIC-DomeBayer Schering
Brand mixturesNot Available
Categories
UNII7GR28W0FJI
CAS number4342-03-4
WeightAverage: 182.187
Monoisotopic: 182.091608966
Chemical FormulaC6H10N6O
InChI KeyFDKXTQMXEQVLRF-ZHACJKMWSA-N
InChI
InChI=1S/C6H10N6O/c1-12(2)11-10-6-4(5(7)13)8-3-9-6/h3H,1-2H3,(H2,7,13)(H,8,9)/b11-10+
IUPAC Name
SMILES
CN(C)\N=N\C1=C(N=CN1)C(N)=O
Pharmacology
Indication

For the treatment of metastatic malignant melanoma. In addition, dacarbazine is also indicated for Hodgkin's disease as a secondary-line therapy when used in combination with other antineoplastic agents.

Structured Indications
Pharmacodynamics

Dacarbazine is a synthetic analog of naturally occurring purine precursor 5-amino-1H-imidazole-4-carboxamide (AIC). After intravenous administration of dacarbazine, the volume of distribution exceeds total body water content suggesting localization in some body tissue, probably the liver. Its disappearance from the plasma is biphasic with initial half-life of 19 minutes and a terminal half-life of 5 hours. 1 In a patient with renal and hepatic dysfunctions, the half-lives were lengthened to 55 minutes and 7.2 hours. 1 The average cumulative excretion of unchanged DTIC in the urine is 40% of the injected dose in 6 hours. 1 DTIC is subject to renal tubular secretion rather than glomerular filtration. At therapeutic concentrations dacarbazine is not appreciably bound to human plasma protein.

Mechanism of action

The mechanism of action is not known, but appears to exert cytotoxic effects via its action as an alkylating agent. Other theories include DNA synthesis inhibition by its action as a purine analog, and interaction with SH groups. Dacarbazine is not cell cycle-phase specific.

TargetKindPharmacological actionActionsOrganismUniProt ID
DNANucleotideyes
cross-linking/alkylation
Humannot applicabledetails
DNA polymerase alpha subunit BProteinunknown
other/unknown
HumanQ14181 details
6-phosphogluconate dehydrogenase, decarboxylatingProteinunknown
inhibitor
HumanP52209 details
Related Articles
Absorption

Erratic, slow and incomplete

Volume of distributionNot Available
Protein binding

Less than 5%

Metabolism

Hepatic

Route of elimination

Dacarbazine is subject to renal tubular secretion rather than glomerular filtration. In man, dacarbazine is extensively degraded. Besides unchanged dacarbazine, 5-aminoimidazole -4 carboxamide (AIC) is a major metabolite of dacarbazine excreted in the urine.

Half life

5 hours

ClearanceNot Available
Toxicity

LD50=350mg/kg (orally in mice)

Affected organisms
  • Humans and other mammals
PathwaysNot Available
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions
DrugInteractionDrug group
AbirateroneThe serum concentration of Dacarbazine can be increased when it is combined with Abiraterone.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Dacarbazine.Approved
AzithromycinThe metabolism of Dacarbazine can be decreased when combined with Azithromycin.Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Dacarbazine.Approved, Investigational
BortezomibThe metabolism of Dacarbazine can be decreased when combined with Bortezomib.Approved, Investigational
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Dacarbazine.Approved
CaffeineThe metabolism of Dacarbazine can be decreased when combined with Caffeine.Approved
CarbamazepineThe metabolism of Dacarbazine can be increased when combined with Carbamazepine.Approved, Investigational
CitalopramThe metabolism of Dacarbazine can be decreased when combined with Citalopram.Approved
ClotrimazoleThe metabolism of Dacarbazine can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of adverse effects can be increased when Dacarbazine is combined with Clozapine.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Dacarbazine.Approved, Investigational
Cyproterone acetateThe serum concentration of Dacarbazine can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
DeferasiroxThe serum concentration of Dacarbazine can be increased when it is combined with Deferasirox.Approved, Investigational
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Dacarbazine.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Dacarbazine.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Dacarbazine.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Dacarbazine.Approved
DisulfiramThe metabolism of Dacarbazine can be decreased when combined with Disulfiram.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Dacarbazine.Approved, Investigational
FingolimodDacarbazine may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
FluvoxamineThe metabolism of Dacarbazine can be decreased when combined with Fluvoxamine.Approved, Investigational
G17DTThe risk or severity of adverse effects can be increased when Dacarbazine is combined with G17DT.Investigational
INGN 201The risk or severity of adverse effects can be increased when Dacarbazine is combined with INGN 201.Investigational
INGN 225The risk or severity of adverse effects can be increased when Dacarbazine is combined with INGN 225.Investigational
IsoniazidThe metabolism of Dacarbazine can be decreased when combined with Isoniazid.Approved
LeflunomideThe risk or severity of adverse effects can be increased when Dacarbazine is combined with Leflunomide.Approved, Investigational
LidocaineThe metabolism of Dacarbazine can be decreased when combined with Lidocaine.Approved, Vet Approved
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Dacarbazine.Withdrawn
MexiletineThe metabolism of Dacarbazine can be decreased when combined with Mexiletine.Approved
NatalizumabThe risk or severity of adverse effects can be increased when Dacarbazine is combined with Natalizumab.Approved, Investigational
NevirapineThe metabolism of Dacarbazine can be decreased when combined with Nevirapine.Approved
NicotineThe metabolism of Dacarbazine can be decreased when combined with Nicotine.Approved
OleandrinAnvirzel may decrease the cardiotoxic activities of Dacarbazine.Experimental
OsimertinibThe serum concentration of Dacarbazine can be decreased when it is combined with Osimertinib.Approved
OuabainOuabain may decrease the cardiotoxic activities of Dacarbazine.Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Dacarbazine.Approved, Vet Approved
Peginterferon alfa-2bThe serum concentration of Dacarbazine can be increased when it is combined with Peginterferon alfa-2b.Approved
PhenobarbitalThe metabolism of Dacarbazine can be increased when combined with Phenobarbital.Approved
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Dacarbazine.Approved, Investigational
PrimidoneThe metabolism of Dacarbazine can be increased when combined with Primidone.Approved, Vet Approved
RifampicinThe metabolism of Dacarbazine can be increased when combined with Rifampicin.Approved
RindopepimutThe risk or severity of adverse effects can be increased when Dacarbazine is combined with CDX-110.Investigational
RoflumilastRoflumilast may increase the immunosuppressive activities of Dacarbazine.Approved
RopiniroleThe metabolism of Dacarbazine can be decreased when combined with Ropinirole.Approved, Investigational
SimeprevirThe metabolism of Dacarbazine can be decreased when combined with Simeprevir.Approved
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Dacarbazine.Approved
SorafenibThe serum concentration of Dacarbazine can be decreased when it is combined with Sorafenib.Approved, Investigational
SRP 299The risk or severity of adverse effects can be increased when Dacarbazine is combined with SRP 299.Investigational
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Dacarbazine.Approved, Investigational
TenofovirThe metabolism of Dacarbazine can be decreased when combined with Tenofovir.Approved, Investigational
TeriflunomideThe serum concentration of Dacarbazine can be decreased when it is combined with Teriflunomide.Approved
TheophyllineThe metabolism of Dacarbazine can be decreased when combined with Theophylline.Approved
TiclopidineThe metabolism of Dacarbazine can be decreased when combined with Ticlopidine.Approved
TofacitinibDacarbazine may increase the immunosuppressive activities of Tofacitinib.Approved, Investigational
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Dacarbazine.Approved, Investigational
VemurafenibThe serum concentration of Dacarbazine can be increased when it is combined with Vemurafenib.Approved
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesL01AX04
AHFS Codes
  • 10:00.00
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingTreatmentCancer, Breast / Colon Neoplasms / Lung Cancers / Malignant Neoplasm of Colon / Melanoma / Neoplasms, Breast / Renal Cancers1
1Active Not RecruitingTreatmentLymphoma, Hodgkins1
1CompletedTreatmentAdvanced Melanoma1
1CompletedTreatmentCarcinoid Tumors / Lung Cancer Small Cell Lung Cancer (SCLC) / Melanoma / Parathyroid Carcinoma / Soft Tissue Sarcoma (STS)1
1CompletedTreatmentHodgkins Disease (HD)1
1CompletedTreatmentMelanoma1
1CompletedTreatmentMelanoma Neoplasms1
1CompletedTreatmentStage IV Melanoma1
1Not Yet RecruitingTreatmentHodgkins Disease (HD)1
1RecruitingTreatmentLymphoma, Hodgkins1
1, 2Active Not RecruitingTreatmentMetastatic Melanoma Stage IV1
1, 2CompletedTreatmentMalignant Melanoma2
1, 2CompletedTreatmentMelanoma1
1, 2CompletedTreatmentMetastatic Melanoma1
1, 2CompletedTreatmentSarcomas1
1, 2CompletedTreatmentStage IV Melanoma1
1, 2RecruitingTreatmentAIDS-Related Hodgkin Lymphoma / CD30-Positive Neoplastic Cells Present / Classical Hodgkin Lymphoma / Human Immunodeficiency Virus (HIV) Infections / Stage II Hodgkin Lymphoma / Stage IIA Hodgkin Lymphoma / Stage IIB Hodgkin Lymphoma / Stage III Hodgkin Lymphoma / Stage IIIA Hodgkin Lymphoma / Stage IIIB Hodgkin Lymphoma / Stage IV Hodgkin Lymphoma / Stage IVA Hodgkin Lymphoma / Stage IVB Hodgkin Lymphoma1
1, 2SuspendedTreatmentMelanoma1
1, 2TerminatedTreatmentMelanoma1
1, 2TerminatedTreatmentThyroid Cancers / Tumors, Solid1
2Active Not RecruitingTreatmentAdult Lymphocyte Depletion Hodgkin Lymphoma / Adult Lymphocyte Predominant Hodgkin Lymphoma / Adult Mixed Cellularity Hodgkin Lymphoma / Adult Nodular Sclerosis Hodgkin Lymphoma / Stage II Adult Hodgkin Lymphoma / Stage III Adult Hodgkin Lymphoma / Stage IV Adult Hodgkin Lymphoma1
2Active Not RecruitingTreatmentCiliary Body and Choroid Melanoma, Medium/Large Size / Ciliary Body and Choroid Melanoma, Small Size / Iris Melanoma / Recurrent Intraocular Melanoma1
2Active Not RecruitingTreatmentHodgkins Disease (HD)1
2Active Not RecruitingTreatmentIris Melanoma / Medium/Large Size Posterior Uveal Melanoma / Ocular Melanoma With Extraocular Extension / Recurrent Uveal Melanoma / Small Size Posterior Uveal Melanoma / Stage IV Uveal Melanoma1
2Active Not RecruitingTreatmentLymphoma, Hodgkins4
2Active Not RecruitingTreatmentMalignant Lymphomas1
2Active Not RecruitingTreatmentMalignant Lymphomas / Nonneoplastic Condition1
2Active Not RecruitingTreatmentMalignant Melanoma1
2Active Not RecruitingTreatmentMetastatic Melanoma1
2Active Not RecruitingTreatmentMetastatic Uveal Melanoma1
2Active Not RecruitingTreatmentRecurrent Uveal Melanoma / Stage III Uveal Melanoma / Stage IIIA Uveal Melanoma / Stage IIIB Uveal Melanoma / Stage IIIC Uveal Melanoma / Stage IV Uveal Melanoma1
2CompletedPreventionMelanoma1
2CompletedTreatmentCancers / Melanoma1
2CompletedTreatmentCarcinoma, Melanoma1
2CompletedTreatmentHodgkins Disease (HD) / Human Immunodeficiency Virus (HIV) Infections1
2CompletedTreatmentLeiomyosarcomas / Malignant Peripheral Nerve Sheath Tumour (MPNST) / Sarcomas / Synovial Sarcoma1
2CompletedTreatmentMalignant Lymphomas5
2CompletedTreatmentMalignant Melanoma2
2CompletedTreatmentMalignant Metastatic Melanoma / Melanoma1
2CompletedTreatmentMelanoma5
2CompletedTreatmentMelanoma (Skin)2
2CompletedTreatmentMetastatic Malignant Melanoma1
2CompletedTreatmentMetastatic Melanoma1
2CompletedTreatmentN-Ras Mutated Locally Advanced or Metastasis Malignant Cutaneous Melanoma1
2CompletedTreatmentNeuroblastomas1
2CompletedTreatmentSarcomas2
2CompletedTreatmentStage III Melanoma / Stage IV Melanoma1
2Not Yet RecruitingTreatmentSolitary Fibrous Tumors1
2Not Yet RecruitingTreatmentUveal Melanoma1
2RecruitingTreatmentClassical Hodgkin Lymphoma1
2RecruitingTreatmentHIV-associated Hodgkin Lymphoma / Human Immunodeficiency Virus (HIV) Infections / Stage III Adult Hodgkin Lymphoma / Stage IV Adult Hodgkin Lymphoma1
2RecruitingTreatmentHodgkins Disease (HD)1
2RecruitingTreatmentLymphoma, Hodgkins1
2RecruitingTreatmentMelanoma1
2RecruitingTreatmentStage II Childhood Hodgkin Lymphoma / Stage III Childhood Hodgkin Lymphoma / Stage IV Childhood Hodgkin Lymphoma1
2TerminatedTreatmentMalignant Lymphomas1
2TerminatedTreatmentMelanoma1
2TerminatedTreatmentMelanoma Metastatic1
2TerminatedTreatmentMetastatic Malignant Melanoma / Unresectable Malignant Melanoma1
2TerminatedTreatmentMetastatic Melanoma2
2TerminatedTreatmentRecurrent Adult Soft Tissue Sarcoma / Stage I Adult Soft Tissue Sarcoma / Stage II Adult Soft Tissue Sarcoma / Stage III Adult Soft Tissue Sarcoma1
2TerminatedTreatmentSarcomas1
2Unknown StatusTreatmentHIV-associated Hodgkin Lymphoma1
2Unknown StatusTreatmentHodgkins Disease (HD)1
2Unknown StatusTreatmentMalignant Lymphomas1
2Unknown StatusTreatmentMalignant Melanoma1
2Unknown StatusTreatmentMelanoma1
3Active Not RecruitingTreatmentAdvanced or Metastatic Liposarcoma or Leiomyosarcoma1
3Active Not RecruitingTreatmentCancers1
3Active Not RecruitingTreatmentLymphoma, Hodgkins4
3Active Not RecruitingTreatmentMalignant Lymphomas2
3Active Not RecruitingTreatmentMelanoma1
3Active Not RecruitingTreatmentMetastatic or Unresectable Cutaneous Melanoma1
3Active Not RecruitingTreatmentUnresectable or Metastatic Melanoma1
3CompletedTreatmentAdvanced Liposarcoma or Leiomyosarcoma1
3CompletedTreatmentHodgkins Disease (HD)1
3CompletedTreatmentLymphoma, Hodgkins4
3CompletedTreatmentMalignant Lymphomas2
3CompletedTreatmentMalignant Melanoma2
3CompletedTreatmentMalignant Melanoma / Recurrent Melanoma1
3CompletedTreatmentMelanoma3
3CompletedTreatmentMelanoma (Skin)4
3CompletedTreatmentMelanoma / Skin Cancers1
3CompletedTreatmentMetastatic Melanoma1
3CompletedTreatmentMetastatic / Uveal Melanoma1
3CompletedTreatmentNeuroblastomas1
3CompletedTreatmentRecurrent Melanoma / Stage III Melanoma / Stage IV Melanoma1
3Not Yet RecruitingTreatmentAlveolar Soft Part Sarcoma (ASPS) / Leiomyosarcomas / Soft-Tissue Sarcoma / Synovial Sarcoma1
3Not Yet RecruitingTreatmentLymphoma, Hodgkins1
3RecruitingTreatmentClassical Hodgkin Lymphoma2
3RecruitingTreatmentMelanoma1
3RecruitingTreatmentMetastatic Melanoma1
3RecruitingTreatmentOcular Melanoma1
3TerminatedTreatmentMalignant Lymphomas2
3Unknown StatusTreatmentLymphoma, Hodgkins1
3Unknown StatusTreatmentMalignant Lymphomas2
3Unknown StatusTreatmentMelanoma1
3Unknown StatusTreatmentNeuroblastomas1
4Unknown StatusTreatmentMetastatic Melanoma1
Not AvailableRecruitingTreatmentClassical Hodgkins Lymphoma in Children and Adolescents1
Not AvailableRecruitingTreatmentLymphoma, Hodgkins1
Not AvailableRecruitingTreatmentNeuroblastomas1
Not AvailableUnknown StatusTreatmentMalignant Lymphomas1
Not AvailableUnknown StatusTreatmentMelanoma (Skin)1
Pharmacoeconomics
Manufacturers
  • Abraxis pharmaceutical products
  • App pharmaceuticals llc
  • Bedford laboratories div ben venue laboratories inc
  • Hospira inc
  • Teva parenteral medicines inc
  • Bayer healthcare pharmaceuticals inc
Packagers
Dosage forms
FormRouteStrength
Injection, powder, for solutionIntravenous10 mg/mL
Injection, powder, for solutionIntravenous200 mg/20mL
Powder, for solutionIntravenous600 mg
LiquidIntravenous200 mg
Powder, for solutionIntravenous10 mg
Prices
Unit descriptionCostUnit
Dacarbazine 200 mg vial22.21USD each
Dacarbazine 100 mg vial11.34USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point (°C)205 °CPhysProp
water solubility4220 mg/LNot Available
logP-0.24HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9923
Blood Brain Barrier+0.9382
Caco-2 permeable+0.5278
P-glycoprotein substrateNon-substrate0.6608
P-glycoprotein inhibitor INon-inhibitor0.8478
P-glycoprotein inhibitor IINon-inhibitor0.9363
Renal organic cation transporterNon-inhibitor0.9125
CYP450 2C9 substrateNon-substrate0.7898
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.579
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9496
CYP450 2D6 inhibitorNon-inhibitor0.9413
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.99
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8208
Ames testAMES toxic0.9107
CarcinogenicityNon-carcinogens0.7624
BiodegradationNot ready biodegradable0.9879
Rat acute toxicity1.9602 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9812
hERG inhibition (predictor II)Non-inhibitor0.7856
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as 2-heteroaryl carboxamides. These are compounds containing a heteroaromatic ring that carries a carboxamide group.
KingdomOrganic compounds
Super ClassOrganic acids and derivatives
ClassCarboxylic acids and derivatives
Sub ClassCarboxylic acid derivatives
Direct Parent2-heteroaryl carboxamides
Alternative ParentsCarbonylimidazoles / Vinylogous amides / Heteroaromatic compounds / Primary carboxylic acid amides / Propargyl-type 1,3-dipolar organic compounds / Azacyclic compounds / Organooxygen compounds / Organonitrogen compounds / Organic oxides / Hydrocarbon derivatives
Substituents2-heteroaryl carboxamide / Imidazole-4-carbonyl group / Azole / Imidazole / Heteroaromatic compound / Vinylogous amide / Primary carboxylic acid amide / Azacycle / Organoheterocyclic compound / Organic 1,3-dipolar compound
Molecular FrameworkAromatic heteromonocyclic compounds
External DescriptorsNot Available

Targets

1. DNA
Kind
Nucleotide
Organism
Human
Pharmacological action
yes
Actions
cross-linking/alkylation
General Function:
Used for biological information storage.
Specific Function:
DNA contains the instructions needed for an organism to develop, survive and reproduce.
Molecular Weight:
2.15 x 1012 Da
References
  1. Lonn U, Lohn S: Prevention of dacarbazine damage of human neoplastic cell DNA by aphidicolin. Cancer Res. 1987 Jan 1;47(1):26-30. [PubMed:3098406 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
other/unknown
General Function:
Protein heterodimerization activity
Specific Function:
May play an essential role at the early stage of chromosomal DNA replication by coupling the polymerase alpha/primase complex to the cellular replication machinery.
Gene Name:
POLA2
Uniprot ID:
Q14181
Molecular Weight:
65947.165 Da
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. Lonn U, Lohn S: Prevention of dacarbazine damage of human neoplastic cell DNA by aphidicolin. Cancer Res. 1987 Jan 1;47(1):26-30. [PubMed:3098406 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Phosphogluconate dehydrogenase (decarboxylating) activity
Specific Function:
Catalyzes the oxidative decarboxylation of 6-phosphogluconate to ribulose 5-phosphate and CO(2), with concomitant reduction of NADP to NADPH.
Gene Name:
PGD
Uniprot ID:
P52209
Molecular Weight:
53139.56 Da
References
  1. Akkemik E, Budak H, Ciftci M: Effects of some drugs on human erythrocyte 6-phosphogluconate dehydrogenase: an in vitro study. J Enzyme Inhib Med Chem. 2010 Aug;25(4):476-9. doi: 10.3109/14756360903257900. [PubMed:20235752 ]
  2. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d 24-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 unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP1A1
Uniprot ID:
P04798
Molecular Weight:
58164.815 Da
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. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
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. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
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 or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
Molecular Weight:
56848.42 Da
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. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Drug created on June 13, 2005 07:24 / Updated on June 11, 2017 20:31