General Information of Drug (ID: DMSE3I7)

Drug Name
Gemcitabine Drug Info
Synonyms
Gemcitabine hydrochloride; DDFC; DFdC; DFdCyd; Folfugem; GEO; Gamcitabine; GemLip; Gemcel; Gemcin; Gemcitabina; Gemcitabinum; Gemtro; Gemzar; Zefei; Gemcitabine HCl; Gemcitabine stereoisomer; LY 188011; LY188011; Gemcitabina [INN-Spanish]; Gemcitabinum [INN-Latin]; Gemzar (TN); Gemzar (hydrochloride); Inno-D07001; LY-188011; Gemcitabine (USAN/INN)
Indication
Disease Entry ICD 11 Status REF
Anterior urethra cancer Approved [1]
Biliary tract cancer 2C17 Approved [1]
Carcinoma 2A00-2F9Z Approved [1]
Cervical cancer 2C77.0 Approved [1]
Cholangiocarcinoma 2C12.10 Approved [1]
Fallopian tube neoplasm Approved [1]
Gallbladder carcinoma Approved [1]
Leiomyosarcoma 2B58 Approved [1]
Leukemia Approved [1]
Lung cancer 2C25.0 Approved [1]
MALT lymphoma Approved [1]
Nodal marginal zone lymphoma 2A85.0 Approved [1]
Non-small-cell lung cancer 2C25 Approved [2]
Ovarian disorder Approved [1]
Ovarian neoplasm Approved [1]
Pancreatic adenocarcinoma Approved [1]
Pancreatic ductal carcinoma 2C10.0 Approved [1]
Pancreatic tumour 2C10 Approved [1]
Posterior urethra cancer Approved [1]
Recurrent adult burkitt lymphoma 2A85.6 Approved [1]
Solid tumour/cancer 2A00-2F9Z Approved [3]
Splenic marginal zone lymphoma Approved [1]
Urethral cancer 2C93 Approved [1]
Urinary bladder neoplasm Approved [1]
Middle East Respiratory Syndrome (MERS) 1D64 Preclinical [4]
Severe acute respiratory syndrome (SARS) 1D65 Preclinical [4]
Colon cancer 2B90.Z Investigative [1]
Therapeutic Class
Anticancer Agents
Cross-matching ID
PubChem CID
60750
ChEBI ID
CHEBI:175901
CAS Number
CAS 95058-81-4
TTD Drug ID
DMSE3I7
VARIDT Drug ID
DR00063
INTEDE Drug ID
DR0765

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Ribonucleoside-diphosphate reductase M2 (RRM2) TTBWDI0 RIR2_HUMAN Modulator [5]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Concentrative nucleoside transporter 1 (SLC28A1) DT0EQPW S28A1_HUMAN Approved [6]
Multidrug resistance-associated protein 5 (ABCC5) DTYVM24 MRP5_HUMAN Approved [7]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Approved [8]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytidine aminohydrolase (CDA) DEKEDRC CDD_HUMAN Approved [9]
Cytidine deaminase (cdd) DETX3A5 CDD_ECOLI Approved [10]
Cytidine deaminase (cdd) DEFVABT CDD_KLEP7 Approved [10]
Uridine/cytidine monophosphate kinase (UMPK) DEMPH4I KCY_HUMAN Approved [11]
Cytidine deaminase (cdd) DEYILK4 E0TLJ6_MYCHH Approved [12]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Ribonucleoside-diphosphate reductase M2 (RRM2) DTT RRM2 5.642 5.91 5.365 6.097
Multidrug resistance-associated protein 5 (ABCC5) DTP MRP5 7.631 8.055 7.961 7.695
P-glycoprotein 1 (ABCB1) DTP P-GP 7.009 6.988 7.442 8.135
Concentrative nucleoside transporter 1 (SLC28A1) DTP CNT1 6.939 4.771 5.736 6.651
Uridine/cytidine monophosphate kinase (UMPK) DME CMPK1 8.862 9.073 8.451 9.186
Cytidine aminohydrolase (CDA) DME CDA 6.127 6.541 4.597 4.392
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Anterior urethra cancer
ICD Disease Classification
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Ribonucleoside-diphosphate reductase M2 (RRM2) DTT RRM2 1.66E-04 2.66 1.68
Multidrug resistance-associated protein 5 (ABCC5) DTP MRP5 8.28E-03 6.40E-01 7.46E-01
P-glycoprotein 1 (ABCB1) DTP P-GP 2.74E-01 -2.19E-01 -3.03E-01
Concentrative nucleoside transporter 1 (SLC28A1) DTP CNT1 2.99E-02 -3.24E-01 -1.02E+00
Uridine/cytidine monophosphate kinase (UMPK) DME CMPK1 2.73E-04 5.37E-01 1.41E+00
Cytidine aminohydrolase (CDA) DME CDA 1.62E-05 4.67E-01 8.77E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Gemcitabine FDA Label
2 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
3 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: 4793).
4 Repurposing of clinically developed drugs for treatment of Middle East respiratory syndrome coronavirus infection. Antimicrob Agents Chemother. 2014 Aug;58(8):4885-93.
5 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
6 Pancreatic Cancer Chemoresistance to Gemcitabine. Cancers (Basel). 2017 Nov 16;9(11).
7 Interdependence of gemcitabine treatment, transporter expression, and resistance in human pancreatic carcinoma cells. Neoplasia. 2010 Sep;12(9):740-7.
8 Increased sensitivity to gemcitabine of P-glycoprotein and multidrug resistance-associated protein-overexpressing human cancer cell lines. Br J Cancer. 2003 Jun 16;88(12):1963-70.
9 Equilibrative nucleoside transporter 1 genotype, cytidine deaminase activity and age predict gemcitabine plasma clearance in patients with solid tumours. Br J Clin Pharmacol. 2011 Mar;71(3):437-44.
10 Potential role of intratumor bacteria in mediating tumor resistance to the chemotherapeutic drug gemcitabine. Science. 2017 Sep 15;357(6356):1156-1160.
11 Gemcitabine pharmacogenomics: deoxycytidine kinase and cytidylate kinase gene resequencing and functional genomics. Drug Metab Dispos. 2008 Sep;36(9):1951-9.
12 Mycoplasma hyorhinis-encoded cytidine deaminase efficiently inactivates cytosine-based anticancer drugs. FEBS Open Bio. 2015 Aug 3;5:634-9.