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- Properties
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Overview
| Generic Names: | CBDCA; cis-Diammine(1,1-cyclobutanedicarboxylato)platinum(II) |
|---|---|
| Trade Names: | Paraplatin; Paraplatin-AQ |
| PharmGKB Accession Id: | PA448803 |
Description
An organoplatinum compound that possesses antineoplastic activity. PubChem (source: Drug Bank)
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. (source: Drug Bank)
ATC Therapeutic Category
- L01XA:Platinum compounds
Pharmacology, Interactions, and Contraindications
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. (source: Drug Bank)
Pharmacology
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. (source: Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Protein Binding
Very low (source: Drug Bank)
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 LD<sub>50</sub> 343 mg kg-1; SCN-RAT LD<sub>50</sub> 72 mg kg-1; IPN-MUS LD<sub>50</sub> 118 mg kg-1
(source:
Drug Bank)
Isomeric SMILES Code:
C1CC(C1)(C(=O)O)C(=O)O.[NH2-].[NH2-].[Pt] (source: Drug Bank)
Curated Annotations (
)
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rs2072671
at chr1:20788288
in
CDA
Risk or phenotype-associated allele: CDA*3 and CDA*2 haplotypic alleles (defined by combined SNPs: rs2072671 c.79A p.Lys27, and rs60369023 c.208G p.Ala70) Phenotype: The CDA*3 haplotype (c.79A, p.Lys27/ c.208A, p.Thr70) was associated with increased incidences of grade 3 or higher neutropenia, and decreased clearance of gemcitabine ( p = 0.0017, n = 177) in the patients receiving gemcitabine with fluorouracil (p = 0.029, n = 14), cisplatin (p = 0.030, n = 30), or carboplatin (p = 0.033, n = 16). The CDA*2 haplotype (c.79C, p.Gln27/ c.208G, p.Ala70) showed no significant effect on gemcitabine pharmacokinetics. Study size: subsets of 256. Study population/ethnicity: Patients with pancreatic, lung or mesothelium carcinoma. /Japanese Significance metric(s): p less than 0.03. Type of association: PK; CO; TOX; ADR- Variant Name:
- CDA: c.79A>C, p.Lys27Gln
- Related Drugs:
- carboplatin, cisplatin, fluorouracil, gemcitabine, Platinum compounds
- Related Diseases:
- Drug Toxicity, Lung Neoplasms, Mesothelioma, Neutropenia, Pancreatic Neoplasms
- Evidence:
-
PMID:17194903
-
rs60369023
at chr1:20804061
in
CDA
Risk or phenotype-associated allele: CDA*3 and CDA*2 haplotypic alleles (defined by combined SNPs: rs2072671 c.79A p.Lys27, and rs60369023 c.208G p.Ala70) Phenotype: The CDA*3 haplotype (c.79A, p.Lys27/ c.208A, p.Thr70) was associated with increased incidences of grade 3 or higher neutropenia, and decreased clearance of gemcitabine ( p = 0.0017, n = 177) in the patients receiving gemcitabine with fluorouracil (p = 0.029, n = 14), cisplatin (p = 0.030, n = 30), or carboplatin (p = 0.033, n = 16). The CDA*2 haplotype (c.79C, p.Gln27/ c.208G, p.Ala70) showed no significant effect on gemcitabine pharmacokinetics. Study size: subsets of 256. Study population/ethnicity: Patients with pancreatic, lung or mesothelium carcinoma. /Japanese Significance metric(s): p less than 0.03. Type of association: PK; CO; TOX; ADR- Variant Name:
- CDA: c.208G>A, p.Ala70Thr
- Related Drugs:
- carboplatin, cisplatin, fluorouracil, gemcitabine, Platinum compounds
- Related Diseases:
- Drug Toxicity, Lung Neoplasms, Mesothelioma, Neutropenia, Pancreatic Neoplasms
- Evidence:
-
PMID:17194903
-
rs2032582
at chr7:86998554
in
ABCB1
Patients with epithelial ovarian cancer, with this variant, have been associated with response to taxane- and platinum-based therapy and gastrointestinal toxicity.- Variant Name:
- ABCB1: 2677G>T/A
- Related Drugs:
- carboplatin, cisplatin, docetaxel, paclitaxel, taxanes
- Related Diseases:
- Ovarian Neoplasms
- Evidence:
-
PMID:19203783
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
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ABCB1 |
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Publications, Variants |
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ABCC1 |
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Publications |
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ABCC2 |
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Publications |
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ABCG2 |
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Publications |
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ALDH1A1 |
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Publications |
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ALDH3A1 |
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Publications |
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ATP7A |
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Publications |
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CAMTA1 |
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Publications |
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CDKN1A |
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Publications |
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CYP1B1 |
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Publications |
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CYP2C8 |
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Publications |
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CYP3A4 |
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Publications |
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CYP3A5 |
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Publications |
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DPYD |
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Publications |
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ERCC2 |
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Publications |
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GSTM1 |
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Publications |
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GSTP1 |
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Publications |
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MAPT |
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Publications |
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SLC22A1 |
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Publications |
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SLC22A2 |
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Publications |
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TP53 |
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Publications |
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UGT1A1 |
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Publications |
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XRCC1 |
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Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| ALB |
|
(source: Drug Bank) |
A list of non-curated publications that mention this drug along with other drugs is available.
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
|
|
Carcinoma, Non-Small-Cell Lung |
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Publications |
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Cystitis |
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Publications |
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Drug Toxicity |
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Publications |
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Esophageal Neoplasms |
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Publications |
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Head and Neck Neoplasms |
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Publications |
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Neoplasms |
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Publications |
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Ovarian Neoplasms |
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Publications, Variants |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Curated Phenotype Datasets
These datasets are sorted alphabetically by title.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
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LinkOuts
Common Searches
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.