Drug Information

Drug (ID: DG00611) and It's Reported Resistant Information

• Name: Methylprednisolone
• Synonyms: Methylprednisolone; 83-43-2; Medrol; Metilprednisolone; Medrone; Urbason; 6alpha-Methylprednisolone; Metilbetasone; Medrate; Dopomedrol; Promacortine; Besonia; Medesone; Mesopren; Metastab; Metrisone; Moderin; Noretona; Solomet; Urbasone; Wyacort; Methylprednisolon; Methyleneprednisolone; Metilprednisolone [DCIT]; delta(1)-6alpha-Methylhydrocortisone; 1-Dehydro-6alpha-methylhydrocortisone; Metilprednisolona; Methylprednisolonum; NSC-19987; Methylprednisolonum [INN-Latin]; Metilprednisolona [INN-Spanish]; 6-alpha-Methylprednisolone; Suprametil; Medrol dosepak; Medrol adt pak; 6alpha-Methyl-11beta,17alpha,21-triol-1,4-pregnadiene-3,20-dione; UNII-X4W7ZR7023; CHEBI:6888; 11beta,17,21-Trihydroxy-6alpha-methylpregna-1,4-diene-3,20-dione; (6alpha,11beta)-11,17,21-Trihydroxy-6-methylpregna-1,4-diene-3,20-dione; (6S,8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-17-(2-hydroxyacetyl)-6,10,13-trimethyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-one; Prednisolone, methyl-; Methylprednisolone, 6-alpha; 11beta,17alpha,21-Trihydroxy-6alpha-methyl-1,4-pregnadiene-3,20-dione; 6alpha-Methylprednisolone base; U 7532; MLS000028541; (6S,8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-17-(2-hydroxyacetyl)-6,10,13-trimethyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one; Sieropresol; Esametone; Firmacort; Medixon; Metrocort; Metysolon; Nirypan; Reactenol; Artisone-wyeth; X4W7ZR7023; MEPRDL; Predni N Tablinen; Medlone 21; SMR000058330; 6alpha-Methyl-11beta,17alpha,21-trihydroxy-1,4-pregnadiene-3,20-dione; DSSTox_CID_3300; Pregna-1,4-diene-3,20-dione, 11,17,21-trihydroxy-6-methyl-, (6a,11b)-; Prednol- L; DSSTox_RID_76965; DSSTox_GSID_23300; Depo-Medrol (acetate); Summicort; CAS-83-43-2; Prednisolone, 6alpha-methyl-; HSDB 3127; MLS002638721; EINECS 201-476-4; Prednisolone, 6.alpha.-methyl-; BRN 2340300; delta(sup 1)-6-alpha-Methylhydrocortisone; .DELTA.1-6.alpha.-Methylhydrocortisone; NCGC00016330-01; Prestwick_622; Medrol (TN); Pregna-1,4-diene-3,20-dione, 11,17,21-trihydroxy-6-methyl-, (6alpha,11beta)-; 6 -Methylprednisolone; Methylprednisolone [USP:INN:BAN:JAN]; Opera_ID_1576; Prestwick0_000279; Prestwick1_000279; Prestwick2_000279; Prestwick3_000279; 6alpha-methyl prednisolone; 11-beta,17,21-Trihydroxy-6-alpha-methylpregna-1,4-diene-3,20-dione; Pregna-1,4-diene-3,20-dione, 11beta,17,21-trihydroxy-6alpha-methyl-; CHEMBL650; EC 201-476-4; 6.alpha.-Methylprednisolone; SCHEMBL5084; BSPBio_000158; 4-08-00-03498 (Beilstein Handbook Reference); MLS001148159; MLS002207191; SPBio_002377; BPBio1_000174; GTPL7088; DTXSID7023300; HMS1568H20; HMS2090B13; HMS2095H20; HMS2230D16; HMS3259J04; HMS3712H20; 6alpha-Methylprednisolone, >=98%; HY-B0260; NSC19987; ZINC3875560; Tox21_110376; Tox21_302018; BDBM50103616; LMST02030178; Methylprednisolone (JP17/USP/INN); MFCD00010591; s1733; AKOS015969744; Pregna-1,4-diene-3,20-dione, 6-alpha-methyl-11-beta-17,21-trihydroxy-; Tox21_110376_1; CCG-220279; DB00959; J3.872E; KS-1273; NC00691; NCGC00022735-03; NCGC00022735-06; NCGC00255269-01; H972; NCI60_001657; M1665; C16437; D00407; 010M591; A855290; Q417222; SR-01000003089; Q-201395; SR-01000003089-2; BRD-K35240538-001-03-1; BRD-K35240538-001-11-4; BRD-K35240538-001-26-2; 6-alpha-Methylprednisolone 100 microg/mL in Acetonitrile; 6alpha-Methylprednisolone, VETRANAL(TM), analytical standard; 11 ,17 ,21-Trihydroxy-6 -methyl-1,4-pregnadiene-3,20-dione; 11beta,17,21-trihydroxy-6alpha-methyl-1,4-pregnadiene-3,20-dione; Methylprednisolone, British Pharmacopoeia (BP) Reference Standard; Methylprednisolone, European Pharmacopoeia (EP) Reference Standard; Pregna-1,20-dione, 11.beta.,17,21-trihydroxy-6.alpha.-methyl-; Pregna-1,20-dione, 6.alpha.-methyl-11.beta.-17,21-trihydroxy-; (6 ,11 )-11,17,21-Trihydroxy-6-methylpregna-1,4-diene-3,20-dione; (6a,11b)-11,17,21-Trihydroxy-6-methylpregna-1,4-diene-3,20-dione; 11beta,17alpha,21-Trihydroxy-6alpha-methylpregna-1,4-diene-3,20-dione; Methylprednisolone, United States Pharmacopeia (USP) Reference Standard; Methylprednisolone for system suitability A, EuropePharmacopoeia (EP) Reference Standard; Methylprednisolone for system suitability, European Pharmacopoeia (EP) Reference Standard; Methylprednisolone, Pharmaceutical Secondary Standard; Certified Reference Material; Pregna-1,20-dione, 11,17,21-trihydroxy-6-methyl-, (6.alpha.,11.beta.)-; Pregna-1,4-diene-3,20-dione, 11,17,21-trihydroxy-6-methyl-, (6I+/-,11I(2))-; Pregna-1,4-diene-3,20-dione, 11beta,17,21-trihydroxy-6alpha-methyl- (8CI)
• Indication:
  In total 2 Indication(s)
  Solid tumour/cancer [ICD-11: 2A00-2F9Z]; Approved; [1]
  Spinal cord injury [ICD-11: 8C21]; Approved; [1]
• Drug Resistance Disease(s):
  Disease(s) with Clinically Reported Resistance for This Drug (1 diseases)
  Rheumatoid arthritis [ICD-11: FA20]; [1]
• Target: Glucocorticoid receptor (NR3C1); GCR_HUMAN; [1]
• Formula: C22H30O5
• IsoSMILES: C[C@H]1C[C@H]2[C@@H]3CC[C@@]([C@]3(C[C@@H]([C@@H]2[C@@]4(C1=CC(=O)C=C4)C)O)C)(C(=O)CO)O
• InChI: 1S/C22H30O5/c1-12-8-14-15-5-7-22(27,18(26)11-23)21(15,3)10-17(25)19(14)20(2)6-4-13(24)9-16(12)20/h4,6,9,12,14-15,17,19,23,25,27H,5,7-8,10-11H2,1-3H3/t12-,14-,15-,17-,19+,20-,21-,22-/m0/s1
• InChIKey: VHRSUDSXCMQTMA-PJHHCJLFSA-N
• PubChem CID: 6741
• ChEBI ID: CHEBI:6888
• TTD Drug ID: D08PIQ
• VARIDT ID: DR00128
• INTEDE ID: DR1056
• DrugBank ID: DB00959

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-15: Musculoskeletal/connective-tissue diseases

Rheumatoid arthritis [ICD-11: FA20]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Irregularity in Drug Uptake and Drug Efflux (IDUE)

Key Molecule: Multidrug resistance protein 1 (ABCB1) [1]

• Molecule Alteration: Expression; Up-regulation
• Resistant Disease: Rheumatoid arthritis [ICD-11: FA20.0]
• Experimental Note: Identified from the Human Clinical Data
• Mechanism Description: MTX is a substrate for eight ABC transporters. In vitro studies demonstrated that RAFLS treated with MTX had higher ABCB1 expression levels than controls, with a positive correlation between ABCB1 expression levels and RA treatment duration. In addition to MTX, other DMARDs (e.g. sulfasalazine, leflunomide, bucillamine, azathioprine), glucocorticoids (e.g. betamethasone, dexamethasone), and NSAIDs (e.g. celecoxib and indomethacin) are also substrates of ABC transporters.

References

• Ref 1: Drug-resistance in rheumatoid arthritis: the role of p53 gene mutations, ABC family transporters and personal factors .Curr Opin Pharmacol. 2020 Oct;54:59-71. doi: 10.1016/j.coph.2020.08.002. Epub 2020 Sep 14. 10.1016/j.coph.2020.08.002