Drug (ID: DG00203) and It's Reported Resistant Information
Name
Rosuvastatin
Synonyms
Astende; Cirantan; Cresadex; Creston; Crestor; Provisacor; Razel; Rosedex; Rosimol; Rosumed; Rosustatin; Rosuvas; Rosuvast; Rosvel; Rovartal; Simestat; Sinlip; Vivacor; Rosuvastatin [INN]; Rosuvastatin calcium; Rosuvastatin calcium [USAN]; Rosuvastatin hemicalcium; S 4522; ZD 4522; ZD4522; AZD-4522; Creston (TN);Crestor (TN); Pyrimidine Compound, 26; Rosuvastatin (INN); S-4522; ZD 4522, calcium salt; ZD-4522; Rosuvastatin calcium (JAN/USAN); Bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino] pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhelpt-6-enoic acid] calcium salt; Calcium (E,3R,5S)-7-[4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-propan-2-ylpyrimidin-5-yl]-3,5-dihydroxyhept-6-enoate; (3R,5S,6E)-7-(4-(4-fluorophenyl)-6-(1-methylethyl)-2-(ethyl(methylsulfonyl)amino)-5-pyrimidinyl)-3,5-dihydroxy-6-heptenoic acid; (3R,5S,6E)-7-{4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-(propan-2-yl)pyrimidin-5-yl}-3,5-dihydroxyhept-6-enoic acid; (3R,5S,6E)-7-{4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl}-3,5-dihydroxyhept-6-enoic acid; (E,3R,5R)-7-[4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-propan-2-ylpyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic acid; (E,3R,5S)-7-[4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-propan-2-ylpyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic acid; (S-((R*,S*-(E)))-7-(4-(4-fluorophenyl)-6-(1-methylethyl)-2-(methyl(methylsulfonyl) amino)-5-pyrimidinyl)-3,5-dihydroxy-6-heptenoic acid, calcium salt (2:1); (S-(R*,S*-(E)))-7-(4-(4-Fluorophenyl)-6-(1-methylethyl)-2-(methyl(methylsulfonyl)amino)-5-pyrimidinyl)-3,5-dihydroxy-6-heptenoic acid, calcium salt (2:1); 6-Heptenoic acid, 7-(4-(4-fluorophenyl)-6-(1-methylethyl)-2-(ethyl(methylsulfonyl)amino)-5-pyrimidinyl)-3,5-dihydroxy-, (3R,5S,6E); 6-Heptenoic acid, 7-(4-(4-fluorophenyl)-6-(1-methylethyl)-2-(methyl(methylsulfonyl)amino)-5-pyrimidinyl)-3,5-dihydroxy-, calcium salt (2:1), (3R,5S,6E)
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Indication
In total 2 Indication(s)
Hyperlipoproteinaemia [ICD-11: 5C80]
Approved
[1], [2]
Blood/blood-forming organ sympton [ICD-11: MA14]
Phase 3
[1], [2]
Structure
Target HMG-CoA reductase (HMGCR) HMDH_HUMAN [1]
Click to Show/Hide the Molecular Information and External Link(s) of This Drug
Formula
C22H28FN3O6S
IsoSMILES
CC(C)C1=NC(=NC(=C1/C=C/[C@H](C[C@H](CC(=O)O)O)O)C2=CC=C(C=C2)F)N(C)S(=O)(=O)C
InChI
1S/C22H28FN3O6S/c1-13(2)20-18(10-9-16(27)11-17(28)12-19(29)30)21(14-5-7-15(23)8-6-14)25-22(24-20)26(3)33(4,31)32/h5-10,13,16-17,27-28H,11-12H2,1-4H3,(H,29,30)/b10-9+/t16-,17-/m1/s1
InChIKey
BPRHUIZQVSMCRT-VEUZHWNKSA-N
PubChem CID
446157
ChEBI ID
CHEBI:38545
TTD Drug ID
D0JE2E
VARIDT ID
DR00223
INTEDE ID
DR1445
DrugBank ID
DB01098
Type(s) of Resistant Mechanism of This Drug
  IDUE: Irregularity in Drug Uptake and Drug Efflux
Drug Resistance Data Categorized by Their Corresponding Diseases
ICD-05: Endocrine/nutritional/metabolic diseases
Click to Show/Hide the Resistance Disease of This Class
Hyperlipoproteinaemia [ICD-11: 5C80]
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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
       Irregularity in Drug Uptake and Drug Efflux (IDUE) Click to Show/Hide
Key Molecule: ATP-binding cassette sub-family G2 (ABCG2) [1], [2]
Molecule Alteration Expression
Down-regulation
Sensitive Disease Hyperlipidemia [ICD-11: 5C80.Z]
Experimental Note Identified from the Human Clinical Data
Experiment for
Molecule Alteration
qPCR
Mechanism Description Enasidenib (and its metabolite, AGI-16903) at clinically relevant concentrations has effects on multiple drug metabolic enzymes and transporters, including inhibition of P-gp, BCRP, OATP1B1, and OATP1B3 transporters. When a single dose of rosuvastatin was administered together with 28 days of dosing of enasidenib, the AUC0-30 and AUC0-inf of rosuvastatin increased by =249% and 244%, respectively; and the Cmax increased by 366%, when compared to the single dose of rosuvastatin administered alone.
Key Molecule: Solute carrier family 21 member 6 (SLC21A6) [2]
Molecule Alteration Expression
Down-regulation
Sensitive Disease Hyperlipidemia [ICD-11: 5C80.Z]
Experimental Note Identified from the Human Clinical Data
Mechanism Description Enasidenib (and its metabolite, AGI-16903) at clinically relevant concentrations has effects on multiple drug metabolic enzymes and transporters, including inhibition of P-gp, BCRP, OATP1B1, and OATP1B3 transporters. When a single dose of rosuvastatin was administered together with 28 days of dosing of enasidenib, the AUC0-30 and AUC0-inf of rosuvastatin increased by =249% and 244%, respectively; and the Cmax increased by 366%, when compared to the single dose of rosuvastatin administered alone.
Key Molecule: Solute carrier family 21 member 8 (SLC21A8) [2]
Molecule Alteration Expression
Down-regulation
Sensitive Disease Hyperlipidemia [ICD-11: 5C80.Z]
Experimental Note Identified from the Human Clinical Data
Mechanism Description Enasidenib (and its metabolite, AGI-16903) at clinically relevant concentrations has effects on multiple drug metabolic enzymes and transporters, including inhibition of P-gp, BCRP, OATP1B1, and OATP1B3 transporters. When a single dose of rosuvastatin was administered together with 28 days of dosing of enasidenib, the AUC0-30 and AUC0-inf of rosuvastatin increased by =249% and 244%, respectively; and the Cmax increased by 366%, when compared to the single dose of rosuvastatin administered alone.
References
Ref 1 Characterization of the Human Intestinal Drug Transport with Ussing Chamber System Incorporating Freshly Isolated Human Jejunum. Drug Metab Dispos. 2021 Jan;49(1):84-93. doi: 10.1124/dmd.120.000138. Epub 2020 Oct 21.
Ref 2 Assessment of Transporter-Mediated Drug Interactions for Enasidenib Based on a Cocktail Study in Patients With Relapse or Refractory Acute Myeloid Leukemia or Myelodysplastic Syndrome. J Clin Pharmacol. 2022 Apr;62(4):494-504. doi: 10.1002/jcph.1979. Epub 2021 Oct 27.

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