General Information of Drug (ID: DMGW1ID)

Drug Name
Sirolimus Drug Info
Synonyms
53123-88-9; Rapamune; Rapamycin (Sirolimus); AY-22989; Rapammune; sirolimusum; WY-090217; RAPA; Antibiotic AY 22989; AY 22989; UNII-W36ZG6FT64; CCRIS 9024; CHEBI:9168; SILA 9268A; W36ZG6FT64; HSDB 7284; C51H79NO13; NSC 226080; DE-109; NCGC00021305-05; DSSTox_CID_3582; DSSTox_RID_77091; DSSTox_GSID_23582; Cypher; Supralimus; Wy 090217; Perceiva; RAP; RPM; Rapamycin from Streptomyces hygroscopicus; SIIA 9268A; LCP-Siro; MS-R001; Rapamune (TN); Rapamycin (TN); Sirolimus (RAPAMUNE); Rapamycin C-7, analog 4; Sirolimus (USAN/INN); Sirolimus [USAN:BAN:INN]; Sirolimus, Rapamune,Rapamycin; Heptadecahydro-9,27-dihydroxy-3-[(1R)-2-[(1S,3R,4R)-4-hydroxy; 23,27-Epoxy-3H-pyrido(2,1-c)(1,4)oxaazacyclohentriacontine; 23,27-Epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine; 23,27-epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine-1,5,11,28,29; 3H-pyrido(2,1-c)(1,4)oxaazacyclohentriacontine-1,5,11,28,29(4H,6H,31H)-pentone; Sirolimus (MTOR inhibitor)
Indication
Disease Entry ICD 11 Status REF
Advanced cancer 2A00-2F9Z Approved [1]
Brainstem neoplasm Approved [1]
Graft-versus-host disease 4B24 Approved [1]
Intracranial meningioma Approved [1]
Lung cancer 2C25.0 Approved [1]
Lung lymphangioleiomyomatosis Approved [1]
Lymphangioleiomyomatosis CB07 Approved [2]
Mucosal melanoma Approved [1]
Multiple myeloma 2A83 Approved [3]
Multiple sclerosis 8A40 Approved [1]
Non-small-cell lung cancer 2C25.Y Approved [1]
Organ transplant rejection NE84 Approved [4]
Plasma cell myeloma 2A83.1 Approved [1]
Prostate cancer 2C82.0 Approved [1]
Salivary gland squamous cell carcinoma Approved [1]
Uveitis 9A96.Z Phase 3 [5]
Coronavirus Disease 2019 (COVID-19) 1D6Y Phase 2 [6]
Dutch elm disease 8D64 Phase 1/2 [4]
Castration-resistant prostate carcinoma Investigative [1]
Neuroblastoma 2D11.2 Investigative [1]
Pancreatic acinar cell carcinoma Investigative [1]
Polycystic kidney disease GB8Y Investigative [1]
Rheumatoid arthritis FA20 Investigative [1]
Therapeutic Class
Immunosuppressive Agents
Cross-matching ID
PubChem CID
5284616
ChEBI ID
CHEBI:9168
CAS Number
CAS 53123-88-9
TTD Drug ID
DMGW1ID
VARIDT Drug ID
DR00262
INTEDE Drug ID
DR1489
ACDINA Drug ID
D00627

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

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Serine/threonine-protein kinase mTOR (mTOR) DTT MTOR 5.425 4.35 5.106 5.188
P-glycoprotein 1 (ABCB1) DTP P-GP 7.009 6.988 7.442 8.135
Organic anion transporting polypeptide 1B1 (SLCO1B1) DTP OATP1B1 9.79 0.485 3.511 2.07
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 10.08 7.207 5.403 9.211
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 11.692 6.58 4.984 9.089
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

References

1 Sirolimus FDA Label
2 FDA Approved Drug Products from FDA Official Website. 2019. Application Number: (ANDA) 201578.
3 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
4 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: 6031).
5 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
6 ClinicalTrials.gov (NCT04341675) Sirolimus Treatment in Hospitalized Patients With COVID-19 Pneumonia. U.S. National Institutes of Health.
7 The genomic landscape of nasopharyngeal carcinoma.Nat Genet. 2014 Aug;46(8):866-71.
8 Knockouts model the 100 best-selling drugs--will they model the next 100 Nat Rev Drug Discov. 2003 Jan;2(1):38-51.
9 Network-based drug repurposing for novel coronavirus 2019-nCoV/SARS-CoV-2. Cell Discov. 2020 Mar 16;6:14.
10 Pharmacokinetic and pharmacodynamic interactions between the immunosuppressant sirolimus and the lipid-lowering drug ezetimibe in healthy volunteers. Clin Pharmacol Ther. 2010 Jun;87(6):663-7.
11 Pharmacogenetics of tacrolimus and sirolimus in renal transplant patients: from retrospective analyses to prospective studies. Transplant Proc. 2007 Sep;39(7):2142-4.
12 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
13 Drug Interactions Flockhart Table