Drug Details

General Information of the Drug (ID: DR3943)
Name
Carboplatin
Synonyms
Azanide; Carbopaltin; Carboplatine; Carboplatino; Carboplatinum; Cbdca; Ercar; Paraplatin; Carboplatine [French]; Carboplatino [Spanish]; Carboplatinum [Latin]; C 2538; JM 8; Carboplatin (USAN); IUPAC: Azane; JM-8; Paraplatin (TN); Paraplatin, Carboplatin; Paraplatin-AQ; Cis-Diammine(cyclobutanedicarboxylato)platinumII; Platinum(+2) Cation; Carboplatin (JAN/USP/INN); Carboplatin [USAN:INN:BAN:JAN]; Cyclobutane-1,1-dicarboxylate; Cyclobutane-1,1-dicarboxylic acid; Diammine-1,1-cyclobutane dicarboxylate platinum II; Cis-Diamine[1,1-cyclobutanedicarboxylato]platinum(II); Cis-Diammine(1,1-cyclobutanedicarboxylato) platinum; Cis-Diammine(1,1-cyclobutanedicarboxylato)platinum; Cis-Diammine[1,1-cyclobutane-dicarboxylato] platinum; Diammine(1,1-cyclobutanedicarboxylato)platinum (II); Platinum, {diammine[1,1-cyclobut; Cis-(1,1-Cyclobutanedicarboxylato)diammineplatinum(II); Cis-Diamine(1,1-cyclobutanedicarboxylato)platinum(II); Cis-Diammine(1,1-cyclobutanedicarboxylato)platinum(II); Platinum(II), (1, 1-cyclobutanedicar; Diammine[cyclobutane-1,1-dicarboxylato(2-)-k2O1,O1]platinum; Diammine(cyclobutane-1,1-dicarboxylato(2-)-O,O')platinum; Platinum, diammine(1,1-cyclobutanedicarboxylato(2-)-O,O')-, (SP-4-2); (SP-4-2)-diammine[cyclobutane-1,1-dicarboxylato(2-)-kappa(2)O,O']platinum; 1,1-Cyclobutanedicarboxylate diammine platinum (II); 1,1-Cyclobutanedicarboxylate diammine platinum(II)
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Molecular Type
Small molecule
Disease Ovarian cancer [ICD-11: 2C73] Approved [1]
Structure
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2D MOL

3D MOL

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Formula
C6H12N2O4Pt
PubChem CID
426756
Canonical SMILES
C1CC(C1)(C(=O)O)C(=O)O.[NH2-].[NH2-].[Pt+2]
InChI
1S/C6H8O4.2H2N.Pt/c7-4(8)6(5(9)10)2-1-3-6;;;/h1-3H2,(H,7,8)(H,9,10);2*1H2;/q;2*-1;+2
InChIKey
VSRXQHXAPYXROS-UHFFFAOYSA-N
CAS Number
CAS 41575-94-4
ChEBI ID
CHEBI:31355
TTD Drug ID
D0X7HM
DrugBank ID
DB00958
Combinatorial Therapeutic Effect(s) Validated Clinically or Experimentally
    α. A List of Natural Product(s) Able to Enhance the Efficacy of This Drug
          Celastrol      Celastrus strigillosus     Click to Show/Hide the Molecular Data of This NP
                 Achieving Therapeutic Synergy     Click to Show/Hide
                    Representative Experiment Reporting the Effect of This Combination [2]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Molecule(s)
                    Regulation		 Induction Degradation FANCD2  Molecule Info 
Pathway MAP
                    In-vitro Model HSJD-DIPG-07 CVCL_VU70 Diffuse intrinsic pontine glioma Homo sapiens
JHH-DIPG-1 CVCL_IT47 Diffuse intrinsic pontine glioma Homo sapiens
SU-DIPG-IV CVCL_IT39 Diffuse intrinsic pontine glioma Homo sapiens
SU-pcGBM-2 CVCL_IT42 Glioblastoma Homo sapiens
VUMC-DIPG-10 Pediatric high-grade gliomas Homo sapiens
VUMC-DIPG-F Pediatric high-grade gliomas Homo sapiens
VUMC-DIPG-G Pediatric high-grade gliomas Homo sapiens
VUMC-HGG-09 Pediatric high-grade gliomas Homo sapiens
VUMC-HGG-14 Pediatric high-grade gliomas Homo sapiens
VUMC-HGG-11 Pediatric high-grade gliomas Homo sapiens
                    In-vivo Model VUMC-HGG-14 cells (50*104 cells in 5 uL) were stereotactically injected into the striatum (4-week old female athymic nude mice).
                    Experimental
                    Result(s)		 Celastrol-induced degradation of FANCD2 sensitizes pediatric high-grade gliomas to the DNA-crosslinking agent carboplatin.
          Curcumin      Hellenia speciosa     Click to Show/Hide the Molecular Data of This NP
                 Achieving Therapeutic Synergy     Click to Show/Hide
                    Representative Experiment Reporting the Effect of This Combination [3]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Molecule(s)
                    Regulation		 Down-regulation Phosphorylation AKT1  Molecule Info 
Pathway MAP
Up-regulation Expression BAX  Molecule Info 
Pathway MAP
Down-regulation Expression BCL-2  Molecule Info 
Pathway MAP
Up-regulation Cleavage CASP3  Molecule Info 
Pathway MAP
Up-regulation Cleavage CASP9  Molecule Info 
Pathway MAP
Up-regulation Expression CDKN1A  Molecule Info 
Pathway MAP
Up-regulation Phosphorylation ERK1  Molecule Info 
Pathway MAP
Up-regulation Phosphorylation ERK2  Molecule Info 
Pathway MAP
Down-regulation Expression MMP-2  Molecule Info 
Pathway MAP
Down-regulation Expression MMP-9  Molecule Info 
Pathway MAP
Down-regulation Expression p105  Molecule Info 
Pathway MAP
Up-regulation Expression TP53  Molecule Info 
Pathway MAP
                    In-vitro Model A-549 CVCL_0023 Lung adenocarcinoma Homo sapiens
                    Experimental
                    Result(s)		 Combined treatment with curcumin and carboplatin inhibited tumor cell growth, migration, and invasion compared with either drug alone. The synergistic antitumor activity of curcumin combined with carboplatin is mediated by multiple mechanisms involving suppression of NF-kappaB via inhibition of the Akt/IKKalpha pathway and enhanced ERK1/2 activity.
          Vanadium      Vanadinite     Click to Show/Hide the Molecular Data of This NP
                 Achieving Therapeutic Synergy     Click to Show/Hide
                    Representative Experiment Reporting the Effect of This Combination [4]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Biological
                    Regulation		 Induction Cell cycle arrest in G0/G1 phase
                    In-vitro Model A-549 CVCL_0023 Lung adenocarcinoma Homo sapiens
MDA-231 Breast cancer Homo sapiens
                    Experimental
                    Result(s)		 Combination of vanadium and carboplatin resulted in synergistic antitumor activity in ex vivo cell cultures, and prompted G0/G1 cell cycle arrest and sensitization of tumor cells to carboplatin-induced apoptosis.
Target and Pathway
Target(s) Human Deoxyribonucleic acid (hDNA)  Molecule Info  [5]
References
Reference 1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7624).
Reference 2 Celastrol-induced degradation of FANCD2 sensitizes pediatric high-grade gliomas to the DNA-crosslinking agent carboplatin. EBioMedicine. 2019 Dec;50:81-92.
Reference 3 Curcumin sensitizes human lung cancer cells to apoptosis and metastasis synergistically combined with carboplatin. Exp Biol Med (Maywood). 2015 Nov;240(11):1416-25.
Reference 4 In vitro and ex vivo vanadium antitumor activity in (TGF-Beta)-induced EMT. Synergistic activity with carboplatin and correlation with tumor metastasis in cancer patients. Int J Biochem Cell Biol. 2016 May;74:121-34.
Reference 5 Inhibition of carboplatin-induced DNA interstrand cross-link repair by gemcitabine in patients receiving these drugs for platinum-resistant ovarian cancer.Clin Cancer Res.2010 Oct 1;16(19):4899-905.
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