Adverse Drug Reaction Classification System

Pharmaceutical Information
Drug Name Sirolimus
Drug ID BADD_D02028
Description Sirolimus, also known as rapamycin, is a macrocyclic lactone antibiotic produced by bacteria _Streptomyces hygroscopicus_, which was isolated from the soil of the Vai Atari region of Rapa Nui (Easter Island).[A242412] It was first isolated and identified as an antifungal agent with potent anticandida activity; however, after its potent antitumor and immunosuppressive activities were later discovered, it was extensively investigated as an immunosuppressive and antitumour agent.[A13448] Its primary mechanism of action is the inhibition of the mammalian target of rapamycin (mTOR), which is a serine/threonine-specific protein kinase that regulates cell growth, proliferation, and survival. mTOR is an important therapeutic target for various diseases, as it was shown to regulate longevity and maintain normal glucose homeostasis.[A242417] Targeting mTOR received more attention especially in cancer, as mTOR signalling pathways are constitutively activated in many types of human cancer.[A1320] Sirolimus was first approved by the FDA in 1999 for the prophylaxis of organ rejection in patients aged 13 years and older receiving renal transplants.[A242372] In November 2000, the drug was recognized by the European Agency as an alternative to calcineurin antagonists for maintenance therapy with corticosteroids.[A242412] In May 2015, the FDA approved sirolimus for the treatment of patients with lymphangioleiomyomatosis.[L39292] In November 2021, albumin-bound sirolimus for intravenous injection was approved by the FDA for the treatment of adults with locally advanced unresectable or metastatic malignant perivascular epithelioid cell tumour (PEComa).[L39267] Sirolimus was also investigated in other cancers such as skin cancer, Kaposi’s Sarcoma, cutaneous T-cell lymphomas, and tuberous sclerosis.[A242372]
Indications and Usage For the prophylaxis of organ rejection in patients receiving renal transplants.
Marketing Status Prescription; Discontinued
ATC Code L04AA10; S01XA23
DrugBank ID DB00877
KEGG ID D00753
MeSH ID D020123
PubChem ID 5284616
TTD Drug ID D03LJR
NDC Product Code 71052-202; 50268-718; 67877-746; 0008-1041; 16714-187; 59573-0004; 67877-748; 59762-1003; 59762-1002; 0008-1042; 73377-024; 60505-6197; 0008-1040; 42513-0013; 55111-654; 55486-1571; 51187-0010; 67877-747; 66689-347; 68382-520; 59762-1205; 55111-653; 42816-1042; 72969-067; 68254-1006; 73683-101; 68462-683; 0904-7147; 16714-188; 68084-915; 80803-153; 42816-1041; 57885-0014; 69238-1594; 42816-1040; 68462-682; 16714-189; 55500-0011; 59762-1001; 0008-1030; 68462-684; 56125-800; 13668-658; 65727-013; 65841-771
Synonyms Sirolimus | Rapamycin | I-2190A | I 2190A | I2190A | AY 22-989 | AY 22 989 | AY 22989 | Rapamune
Chemical Information
Molecular Formula C51H79NO13
CAS Registry Number 53123-88-9
SMILES CC1CCC2CC(C(=CC=CC=CC(CC(C(=O)C(C(C(=CC(C(=O)CC(OC(=O)C3CCCCN3C(=O)C(=O)C1(O2)O) C(C)CC4CCC(C(C4)OC)O)C)C)O)OC)C)C)C)OC
Chemical Structure
ADR Related Proteins Induced by Drug
ADR Term Protein Name UniProt AC TTD Target ID PMID
Adverse drug reactionErythroagglutinating phytohemagglutininP05088Not Available2246324; 2738100; 8880225; 8288727; 2515162; 6831033; 3871216; 1950737; 2548278; 2846698; 3262683; 7759599; 9869836; 2211719; 3131638; 2809200; 2540100; 9287244; 12082550; 7535569
Nephropathy toxicInterleukin-2P60568T616988591053; 7694398; 7592869; 7533090; 7542793; 7524531; 7520696
Nephropathy toxicNuclear receptor ROR-gammaP51449T253078591053; 7694398; 7592869; 7533090; 7542793; 7524531; 7520696
Nephropathy toxicCalcineurin subunit B type 1P63098Not Available8591053; 7694398; 7592869; 7533090; 7542793; 7524531; 7520696
ADRs Induced by Drug
ADR Term ADReCS ID ADR Frequency (FAERS) ADR Severity Grade (FAERS) ADR Severity Grade (CTCAE)
Gastroenteritis07.19.03.001; 11.01.07.0040.000686%Not Available
Gastrointestinal disorder07.11.01.0010.001716%Not Available
Gastrointestinal pain07.01.05.005--
Generalised oedema14.05.06.007; 08.01.07.004--
Gingival hyperplasia07.09.03.002--Not Available
Gingivitis07.09.03.003; 11.01.04.013--
Glycosuria20.02.01.005--
Gout15.01.06.001; 14.09.01.001--Not Available
Graft versus host disease12.02.09.001; 10.02.01.0270.001164%Not Available
Haematochezia07.12.02.003; 24.07.02.0120.001030%Not Available
Haematuria24.07.01.047; 20.02.01.006--
Haemoglobin13.01.05.018--Not Available
Haemoglobin decreased13.01.05.003--Not Available
Haemolytic uraemic syndrome01.06.02.001; 20.01.03.0110.000686%
Haemoptysis24.07.01.006; 22.02.03.004; 02.01.02.0060.000269%Not Available
Hallucination19.10.02.002--
Headache17.14.01.001--
Hepatic artery thrombosis24.01.03.002; 09.01.06.005--Not Available
Hepatic failure09.01.03.0020.000448%
Hepatic necrosis09.01.07.002--
Hepatitis C11.05.06.004; 09.01.09.0050.000686%Not Available
Hepatocellular injury09.01.07.008--Not Available
Hepatotoxicity12.03.01.008; 09.01.07.009--Not Available
Hernia08.01.04.0010.002059%Not Available
Herpes simplex11.05.02.001; 23.09.03.001--Not Available
Herpes zoster23.09.03.002; 11.05.02.0030.001030%
Hiccups22.02.04.002; 07.01.06.009--
Hip fracture15.08.03.001; 12.04.01.0010.000686%
Hirsutism23.02.04.001; 05.05.01.005--
Human herpesvirus 6 infection11.05.02.0200.000686%Not Available
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