Drug Details
| General Information of the Drug (ID: DR0141) | ||||
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| Name |
Oxaliplatin
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| Synonyms |
Eloxatin (TN); Medac (TN); Oxaliplatin (TN); Oxaliplatin (JAN/USAN/INN)
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| Molecular Type |
Small molecule
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| Disease | Colorectal cancer [ICD-11: 2B91] | Approved | [1] | |
| Structure |
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Click to Download Mol2D MOL |
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| ADMET Property |
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability
Clearance
The renal clearance of drug is 10-17 L/h
Half-life
The concentration or amount of drug in body reduced by one-half in 0.43 hours (alpha), and 16.8 hours (beta)
Metabolism
The drug is metabolized via the displacement of the labile oxalate ligand
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 8.1315 micromolar/kg/day
Unbound Fraction
The unbound fraction of drug in plasma is 0.13%
Vd
The volume of distribution (Vd) of drug is 440 L
Water Solubility
The ability of drug to dissolve in water is measured as 6 mg/mL
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| Click to Show/Hide the Molecular Information and External Link(s) of This Natural Product | ||||
| Formula |
C8H14N2O4Pt
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| PubChem CID | ||||
| Canonical SMILES |
C1CCC(C(C1)[NH-])[NH-].C(=O)(C(=O)O)O.[Pt+2]
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| InChI |
1S/C6H12N2.C2H2O4.Pt/c7-5-3-1-2-4-6(5)8;3-1(4)2(5)6;/h5-8H,1-4H2;(H,3,4)(H,5,6);/q-2;;+2/t5-,6-;;/m1../s1
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| InChIKey |
DRMCATBEKSVAPL-BNTLRKBRSA-N
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| CAS Number |
CAS 61825-94-3
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| ChEBI ID | ||||
| GDSC | ||||
| TTD Drug ID | ||||
| DrugBank ID | ||||
| Combinatorial Therapeutic Effect(s) Validated Clinically or Experimentally | ||||||
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| α. A List of Natural Product(s) Able to Enhance the Efficacy of This Drug | ||||||
| Artemisinin | Artemisia annua | 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
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| Molecule(s)
Regulation |
Down-regulation | Expression | BIRC5 | Molecule Info |
Pathway MAP
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| Down-regulation | Expression | CTNNB1 | Molecule Info |
Pathway MAP
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| Down-regulation | Expression | MYC | Molecule Info |
Pathway MAP
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| In-vitro Model | Eca-109 | CVCL_6898 | Esophageal squamous cell carcinoma | Homo sapiens | ||
| Experimental
Result(s) |
Combination treatment with artemisinin and oxaliplatin inhibits tumorigenesis in esophageal cancer EC109 cell through Wnt/beta-catenin signaling pathway. | |||||
| Daunorubicin | Streptomyces peucetius | 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
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| Molecule(s)
Regulation |
Down-regulation | Expression | TOP2A | Molecule Info |
Pathway MAP
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| In-vitro Model | SK-OV-3 | CVCL_0532 | Ovarian serous cystadenocarcinoma | Homo sapiens | ||
| Experimental
Result(s) |
Composite micelles showed reduced systematic toxicity and greater synergistic effect than combination of small molecules of hydrophilic platinum drug Oxa(II) and hydrophobic drug DRB both in vitro and in vivo. | |||||
| Fluoroorotic acid | Homo sapiens | 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
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| In-vivo Model | Clinical trial | |||||
| Experimental
Result(s) |
Combination chemotherapy with oxaliplatin, 5-FU, and FA is an active and well-tolerated regimen as first-line treatment in patients with metastatic or recurrent gastric cancer. | |||||
| Ginsenoside Rg3 | Panax ginseng | 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 | [6] | |||||
| Detail(s) |
Combination Info
click to show the detail info of this combination
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| Molecule(s)
Regulation |
Down-regulation | Expression | CCND1 | Molecule Info |
Pathway MAP
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| Down-regulation | Expression | PCNA | Molecule Info |
Pathway MAP
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| In-vitro Model | SMMC-7721 | CVCL_0534 | Hepatocellular carcinoma | Homo sapiens | ||
| Experimental
Result(s) |
Cells treated with oxaliplatin+ ginsenoside enhanced the anti-tumor effect and may inhibit the proliferation and promoted apoptosis of hepatocellular carcinoma via regulating the expression of PCNA and cyclin D1. | |||||
| Honokiol | Magnolia officinalis | 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 | [7] | |||||
| Detail(s) |
Combination Info
click to show the detail info of this combination
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| Molecule(s)
Regulation |
Down-regulation | Expression | AKT1 | Molecule Info |
Pathway MAP
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| Down-regulation | Expression | ERK1 | Molecule Info |
Pathway MAP
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| Down-regulation | Expression | ERK2 | Molecule Info |
Pathway MAP
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| Down-regulation | Expression | RELA | Molecule Info |
Pathway MAP
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| In-vitro Model | HT-29 | CVCL_0320 | Colon adenocarcinoma | Homo sapiens | ||
| Experimental
Result(s) |
Honokiol augments the anti-cancer effects of oxaliplatin in colon cancer cells. | |||||
| Mangiferin | Mangifera indica | 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 | [8] | |||||
| Detail(s) |
Combination Info
click to show the detail info of this combination
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| Molecule(s)
Regulation |
Up-regulation | Expression | CASP3 | Molecule Info |
Pathway MAP
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| Down-regulation | Expression | p105 | Molecule Info |
Pathway MAP
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| In-vitro Model | HT29 | CVCL_A8EZ | Colorectal adenocarcinoma | Mus musculus | ||
| Experimental
Result(s) |
Mangiferin in combination with oxaliplatin favours apoptotic cell death and thereby improves the efficacy of oxaliplatin in vitro. | |||||
| Neferine | Nelumbo nucifera | 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 | [9] | |||||
| Detail(s) |
Combination Info
click to show the detail info of this combination
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| Molecule(s)
Regulation |
Up-regulation | Expression | CDH1 | Molecule Info |
Pathway MAP
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| Experimental
Result(s) |
Snail overexpression or TGF-Beta1-induced EMT attenuated Neferine-mediated OXA sensitization in HCC. | |||||
| Piperlongumine | Piper longum | 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 | [10] | |||||
| Detail(s) |
Combination Info
click to show the detail info of this combination
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| Molecule(s)
Regulation |
Up-regulation | Expression | BAX | Molecule Info |
Pathway MAP
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| Down-regulation | Expression | BCL-2 | Molecule Info |
Pathway MAP
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| Up-regulation | Activity | CASP3 | Molecule Info |
Pathway MAP
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| In-vitro Model | HCT 116 | CVCL_0291 | Colon carcinoma | Homo sapiens | ||
| LoVo | CVCL_0399 | Colon adenocarcinoma | Homo sapiens | |||
| GES-1 | CVCL_EQ22 | Healthy | Homo sapiens | |||
| In-vivo Model | For a xenograft model, HCT-116 cells (1*107 in 150 uL PBS) were subcutaneously injected into the right flank of five-week-old female athymic BALB/c nu/nu mice. | |||||
| Experimental
Result(s) |
The synergistic effects of oxaliplatin and piperlongumine on colorectal cancer are mediated by oxidative stress. | |||||
| Scutellarin | Scutellaria indica | 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 | [11] | |||||
| Detail(s) |
Combination Info
click to show the detail info of this combination
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| Molecule(s)
Regulation |
Up-regulation | Cleavage | CASP3 | Molecule Info |
Pathway MAP
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| Up-regulation | Cleavage | CASP9 | Molecule Info |
Pathway MAP
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| Down-regulation | Activity | PKM | Molecule Info |
Pathway MAP
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| In-vitro Model | SW480 | CVCL_0546 | Colon adenocarcinoma | Homo sapiens | ||
| HT29 | CVCL_A8EZ | Colorectal adenocarcinoma | Mus musculus | |||
| In-vivo Model | For a xenograft model, 5 * 106 OR-SW480 cells were subcutaneously injected into the right armpit of 4-week-old female immunodeficient nude BALB/c mice. | |||||
| Experimental
Result(s) |
Scutellarin resensitizes oxaliplatin-resistant CRC cells to oxaliplatin treatment through inhibition of PKM2. | |||||
| Sulforaphane | Brassica oleracea | 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 | [12] | |||||
| Detail(s) |
Combination Info
click to show the detail info of this combination
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| Molecule(s)
Regulation |
Up-regulation | Expression | CASP3 | Molecule Info |
Pathway MAP
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| Up-regulation | Expression | PARP1 | Molecule Info |
Pathway MAP
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| In-vitro Model | Caco-2 | CVCL_0025 | Colon adenocarcinoma | Homo sapiens | ||
| Experimental
Result(s) |
SFN and Ox alone inhibited cell growth of Caco-2 cells in a dose-dependent manner, an effect, which could be synergistically enhanced, when cells were incubated with the combination of both agents. | |||||
| Triptolide | Tripterygium hypoglaucum | 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 | [13] | |||||
| Detail(s) |
Combination Info
click to show the detail info of this combination
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| Molecule(s)
Regulation |
Down-regulation | Expression | LEF1 | Molecule Info |
Pathway MAP
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| Down-regulation | Expression | TCF7 | Molecule Info |
Pathway MAP
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| In-vitro Model | SW480 | CVCL_0546 | Colon adenocarcinoma | Homo sapiens | ||
| In-vivo Model | SW480 cells were subcutaneously injected into the back of the mice (2*106 cells in 200 mL of medium). | |||||
| Experimental
Result(s) |
Triptolide synergistically enhances antitumor activity of oxaliplatin in colon carcinoma in vitro and in vivo. | |||||
| Ursolic acid | Potentilla indica | 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 | [14] | |||||
| Detail(s) |
Combination Info
click to show the detail info of this combination
|
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| Molecule(s)
Regulation |
Down-regulation | Phosphorylation | AKT1 | Molecule Info |
Pathway MAP
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| Down-regulation | Phosphorylation | ERK1 | Molecule Info |
Pathway MAP
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| Down-regulation | Phosphorylation | ERK2 | Molecule Info |
Pathway MAP
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| Down-regulation | Phosphorylation | IKKA | Molecule Info |
Pathway MAP
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| In-vitro Model | SW480 | CVCL_0546 | Colon adenocarcinoma | Homo sapiens | ||
| SW620 | CVCL_0547 | Colon adenocarcinoma | Homo sapiens | |||
| LoVo | CVCL_0399 | Colon adenocarcinoma | Homo sapiens | |||
| RKO | CVCL_0504 | Colon carcinoma | Homo sapiens | |||
| In-vivo Model | SW620 cells (1*107) were injected subcutaneously into the right flank area of 6-8-week-old female nude mice. | |||||
| Experimental
Result(s) |
Ursolic acid inhibited proliferation and induced apoptosis of all four cells, enhanced the cytotoxicity of oxaliplatin, and restored liver function and body weight of the mice treated with oxaliplatin. | |||||
| Wogonin | Scutellaria amoena | Click to Show/Hide the Molecular Data of This NP | ||||
| Augmenting Drug Sensitivity | Click to Show/Hide | |||||
| Representative Experiment Reporting the Effect of This Combination | [15] | |||||
| Detail(s) |
Combination Info
click to show the detail info of this combination
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| Molecule(s)
Regulation |
Up-regulation | Phosphorylation | JNK1 | Molecule Info |
Pathway MAP
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| Down-regulation | Phosphorylation | ULK1 | Molecule Info |
Pathway MAP
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| Biological
Regulation |
Up-regulation | Peroxynitrite formation | ||||
| In-vitro Model | BGC-823 | CVCL_3360 | Gastric cancer | Homo sapiens | ||
| In-vivo Model | Approximately 300 cells for the CM-Dil-labeled BGC-823 cells were injected into the yolk sac per zebrafish embryo using a microinjector. | |||||
| Experimental
Result(s) |
Wogonin exacerbates the cytotoxic effect of oxaliplatin by inducing nitrosative stress and autophagy in human gastric cancer cells. | |||||
| β. A List of Natural Product(s) Able to Decrease the Adverse Effect of This Drug | ||||||
| Magnolol | Magnolia officinalis | Click to Show/Hide the Molecular Data of This NP | ||||
| Decreasing Adverse Drug Reaction | Click to Show/Hide | |||||
| Representative Experiment Reporting the Effect of This Combination | [16] | |||||
| Detail(s) |
Combination Info
click to show the detail info of this combination
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| Molecule(s)
Regulation |
Down-regulation | Expression | p105 | Molecule Info |
Pathway MAP
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| Experimental
Result(s) |
MG could prevent the development and progression of mucositis induced by oxaliplatin through multipathway. | |||||
| γ. A List of Natural Product(s) Able to Reverse the Resistance of This Drug | ||||||
| Curcumin | Hellenia speciosa | Click to Show/Hide the Molecular Data of This NP | ||||
| Reversing Drug Resistance | Click to Show/Hide | |||||
| Representative Experiment Reporting the Effect of This Combination | [17] | |||||
| Detail(s) |
Combination Info
click to show the detail info of this combination
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| Molecule(s)
Regulation |
Down-regulation | Expression | BCL-2 | Molecule Info |
Pathway MAP
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| Up-regulation | Cleavage | CASP3 | Molecule Info |
Pathway MAP
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| Down-regulation | Expression | CDH2 | Molecule Info |
Pathway MAP
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| Down-regulation | Phosphorylation | RELA | Molecule Info |
Pathway MAP
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| Down-regulation | Phosphorylation | SMAD2 | Molecule Info |
Pathway MAP
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| Down-regulation | Expression | TGFB1 | Molecule Info |
Pathway MAP
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| In-vitro Model | HCT 116 | CVCL_0291 | Colon carcinoma | Homo sapiens | ||
| SW480 | CVCL_0546 | Colon adenocarcinoma | Homo sapiens | |||
| In-vivo Model | HCT116/OXA cells were transplanted subcutaneously into the right flank in each BALB/c nude mice (6-8 weeks old, 20+/-2 g weight). | |||||
| Experimental
Result(s) |
Curcumin reverses oxaliplatin resistance in human colorectal cancer via regulation of TGF-beta/Smad2/3 signaling pathway. | |||||
| Dicoumarol | Vanilla fragrans | Click to Show/Hide the Molecular Data of This NP | ||||
| Reversing Drug Resistance | Click to Show/Hide | |||||
| Representative Experiment Reporting the Effect of This Combination | [18] | |||||
| Detail(s) |
Combination Info
click to show the detail info of this combination
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| Molecule(s)
Regulation |
Down-regulation | Expression | CYB5R2 | Molecule Info |
Pathway MAP
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| In-vitro Model | SNU-449 | CVCL_0454 | Adult hepatocellular carcinoma | Homo sapiens | ||
| SNU-387 | CVCL_0250 | Adult hepatocellular carcinoma | Homo sapiens | |||
| Experimental
Result(s) |
Dicoumarol enhances gemcitabine-induced cytotoxicity in high NQO1-expressing cholangiocarcinoma cells. | |||||
| Elemene | Pogostemon cablin | Click to Show/Hide the Molecular Data of This NP | ||||
| Reversing Drug Resistance | Click to Show/Hide | |||||
| Representative Experiment Reporting the Effect of This Combination | [19] | |||||
| Detail(s) |
Combination Info
click to show the detail info of this combination
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| Molecule(s)
Regulation |
Down-regulation | Phosphorylation | AKT1 | Molecule Info |
Pathway MAP
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| Up-regulation | Expression | BECN1 | Molecule Info |
Pathway MAP
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| Up-regulation | Cleavage | CASP3 | Molecule Info |
Pathway MAP
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| Down-regulation | Phosphorylation | ERK1 | Molecule Info |
Pathway MAP
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| Up-regulation | Expression | MAP1LC3A | Molecule Info |
Pathway MAP
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| Up-regulation | Cleavage | PAEP | Molecule Info | |||
| In-vitro Model | MHCC97-H | CVCL_4972 | Adult hepatocellular carcinoma | Homo sapiens | ||
| HCCLM3 | CVCL_6832 | Adult hepatocellular carcinoma | Homo sapiens | |||
| In-vivo Model | Human HCC cell line MHCC97H were used to estabolish xenograft models in the BALB/c mice. | |||||
| Experimental
Result(s) |
Beta-elemene sensitizes hepatocellular carcinoma cells to oxaliplatin by preventing oxaliplatin-induced degradation of copper transporter 1. | |||||
| Luteolin | Abrus precatorius | Click to Show/Hide the Molecular Data of This NP | ||||
| Reversing Drug Resistance | Click to Show/Hide | |||||
| Representative Experiment Reporting the Effect of This Combination | [20] | |||||
| Detail(s) |
Combination Info
click to show the detail info of this combination
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| Molecule(s)
Regulation |
Down-regulation | Expression | GABPA | Molecule Info | ||
| Down-regulation | Expression | GSTA1 | Molecule Info |
Pathway MAP
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| Down-regulation | Expression | GSTA2 | Molecule Info |
Pathway MAP
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| Down-regulation | Expression | HMOX1 | Molecule Info |
Pathway MAP
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| Down-regulation | Expression | NQO1 | Molecule Info |
Pathway MAP
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| In-vitro Model | HCT 116 | CVCL_0291 | Colon carcinoma | Homo sapiens | ||
| SW620 | CVCL_0547 | Colon adenocarcinoma | Homo sapiens | |||
| Experimental
Result(s) |
Luteolin sensitizes two oxaliplatin-resistant colorectal cancer cell lines to chemotherapeutic drugs via inhibition of the Nrf2 pathway. | |||||
| Target and Pathway | ||||
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| Target(s) | Epidermal growth factor receptor (EGFR) | Molecule Info | ||
| Human Deoxyribonucleic acid (hDNA) | Molecule Info | [21] | ||
