U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C51H79NO13
Molecular Weight 914.1738
Optical Activity UNSPECIFIED
Defined Stereocenters 15 / 15
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of SIROLIMUS

SMILES

C[C@]1([H])/C(/[H])=C(\[H])/C(/[H])=C(\[H])/C(/[H])=C(\C)/[C@]([H])(C[C@]2([H])CC[C@@]([H])(C)[C@@](C(=O)C(=O)N3CCCC[C@@]3([H])C(=O)O[C@@]([H])(CC(=O)[C@]([H])(C)/C(/[H])=C(\C)/[C@]([H])([C@]([H])(C(=O)[C@]([H])(C)C1)OC)O)[C@]([H])(C)C[C@]4([H])CC[C@]([H])([C@@]([H])(C4)OC)O)(O)O2)OC

InChI

InChIKey=QFJCIRLUMZQUOT-HPLJOQBZSA-N
InChI=1S/C51H79NO13/c1-30-16-12-11-13-17-31(2)42(61-8)28-38-21-19-36(7)51(60,65-38)48(57)49(58)52-23-15-14-18-39(52)50(59)64-43(33(4)26-37-20-22-40(53)44(27-37)62-9)29-41(54)32(3)25-35(6)46(56)47(63-10)45(55)34(5)24-30/h11-13,16-17,25,30,32-34,36-40,42-44,46-47,53,56,60H,14-15,18-24,26-29H2,1-10H3/b13-11+,16-12+,31-17+,35-25+/t30-,32-,33-,34-,36-,37+,38+,39+,40-,42+,43+,44-,46-,47+,51-/m1/s1

HIDE SMILES / InChI

Molecular Formula C51H79NO13
Molecular Weight 914.1738
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 15 / 15
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment:: https://www.ncbi.nlm.nih.gov/pubmed/20005306

Sirolimus is the USAN-assigned generic name for the natural product rapamycin. Sirolimus is produced by a strain of Streptomyces hygroscopicus, isolated from a soil sample collected from Rapa Nui commonly known as Easter Island. Although sirolimus was isolated as an antifungal agent with potent anticandida activity, subsequent studies revealed impressive antitumor and immunosuppressive activities. Sirolimus demonstrates activity against several murine tumors, such as B16 43 melanocarcinoma, Colon 26 tumor, EM ependymoblastoma, and mammary and colon 38 solid tumors. Demonstration of the potent immunosuppressive activity of sirolimus in animal models of organ transplantation led to clinical trials and subsequent approval by regulatory authorities for prophylaxis of renal graft rejection. Interest in sirolimus as an immunosuppressive therapy in organ transplantation derives from its unique mechanism of action, its unique side-effect profile, and its ability to synergize with other immunosuppressive agents. It is used in medicine to prevent organ transplant rejection and to treat lymphangioleiomyomatosis. Sirolimus inhibits T-lymphocyte activation and proliferation that occurs in response to antigenic and cytokine (Interleukin [IL]-2, IL-4, and IL-15) stimulation by a mechanism that is distinct from that of other immunosuppressants. Sirolimus also inhibits antibody production. In cells, sirolimus binds to the immunophilin, FK Binding Protein-12 (FKBP-12), to generate an immunosuppressive complex. This complex blocks the activation of the cell-cycle-specific kinase, TOR. The downstream events that follow the inactivation of TOR result in the blockage of cell-cycle progression at the juncture of G1 and S phase. Rapamycin/FKBP12 efficiently inhibit some, but not all, functions of mTOR and hence much interest has been placed in the development of drugs that target the kinase activity of mTOR directly. Studies in experimental models show that sirolimus prolongs allograft (kidney, heart, skin, islet, small bowel, pancreatico-duodenal, and bone marrow) survival in mice, rats, pigs, and/or primates. Sirolimus reverses acute rejection of heart and kidney allografts in rats and prolongs the graft survival in presensitized rats. In some studies, the immunosuppressive effect of sirolimus lasts up to 6 months after discontinuation of therapy. This tolerization effect is alloantigen-specific. In rodent models of autoimmune disease, sirolimus suppresses immune-mediated events associated with systemic lupus erythematosus, collagen-induced arthritis, autoimmune type I diabetes, autoimmune myocarditis, experimental allergic encephalomyelitis, graft-versus-host disease, and autoimmune uveoretinitis. Lymphangioleiomyomatosis involves lung tissue infiltration with smooth muscle-like cells that harbor inactivating mutations of the tuberous sclerosis complex (TSC) gene (LAM cells). Loss of TSC gene function activates the mTOR signaling pathway, resulting in cellular proliferation and release of lymphangiogenic growth factors. Sirolimus inhibits the activated mTOR pathway and thus the proliferation of LAM cells.

Originator

Curator's Comment:: Rapamycin is a natural product isolated from Streptomyces hygroscopicus, found on the island of Rapa Nui in 1972

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
RAPAMUNE

Approved Use

Rapamune is an immunosuppressive agent indicated for the prophylaxis of organ rejection in patients aged ≥13 years receiving renal transplants. Patients at low- to moderate-immunologic risk: Use initially with cyclosporine (CsA) and corticosteroids. CsA withdrawal is recommended 2-4 months after transplantation ( 1.1 ). Patients at high-immunologic risk: Use in combination with cyclosporine and corticosteroids for the first 12 months following transplantation ( 1.1 ). Safety and efficacy of CsA withdrawal has not been established in high risk patients ( 1.1 , 1.2 , 14.3 ). Therapeutic drug monitoring is recommended for all patients ( 2.3 , 5.14 ). 1.1 Prophylaxis of Organ Rejection in Renal Transplantation Rapamune (sirolimus) is indicated for the prophylaxis of organ rejection in patients aged 13 years or older receiving renal transplants. Therapeutic drug monitoring is recommended for all patients receiving Rapamune [see Dosage and Administration (2.3), Warnings and Precautions (5.14)

Launch Date

937353600000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
78.2 ng/mL
15 mg single, oral
dose: 15 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SIROLIMUS plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
970 ng × h/mL
15 mg single, oral
dose: 15 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SIROLIMUS plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
79 h
15 mg single, oral
dose: 15 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SIROLIMUS plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
6%
15 mg single, oral
dose: 15 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SIROLIMUS plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
40 mg single, oral
Highest studied dose
Dose: 40 mg
Route: oral
Route: single
Dose: 40 mg
Sources:
healthy, 48.5 years (range: 40-63 years)
Health Status: healthy
Age Group: 48.5 years (range: 40-63 years)
Sex: M+F
Sources:
Other AEs: Mouth ulceration, Headache...
Other AEs:
Mouth ulceration (moderate, 1 patient)
Headache (1 patient)
Alanine aminotransferase increase (1 patient)
Sources:
6 mg multiple, oral
Recommended
unhealthy
Other AEs: Immunosuppression, Hepatic artery thrombosis...
Other AEs:
Immunosuppression
Hepatic artery thrombosis
Dehiscence
Sources:
AEs

AEs

AESignificanceDosePopulation
Alanine aminotransferase increase 1 patient
40 mg single, oral
Highest studied dose
Dose: 40 mg
Route: oral
Route: single
Dose: 40 mg
Sources:
healthy, 48.5 years (range: 40-63 years)
Health Status: healthy
Age Group: 48.5 years (range: 40-63 years)
Sex: M+F
Sources:
Headache 1 patient
40 mg single, oral
Highest studied dose
Dose: 40 mg
Route: oral
Route: single
Dose: 40 mg
Sources:
healthy, 48.5 years (range: 40-63 years)
Health Status: healthy
Age Group: 48.5 years (range: 40-63 years)
Sex: M+F
Sources:
Mouth ulceration moderate, 1 patient
40 mg single, oral
Highest studied dose
Dose: 40 mg
Route: oral
Route: single
Dose: 40 mg
Sources:
healthy, 48.5 years (range: 40-63 years)
Health Status: healthy
Age Group: 48.5 years (range: 40-63 years)
Sex: M+F
Sources:
Dehiscence
6 mg multiple, oral
Recommended
unhealthy
Hepatic artery thrombosis
6 mg multiple, oral
Recommended
unhealthy
Immunosuppression
6 mg multiple, oral
Recommended
unhealthy
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG



OverviewOther

Drug as perpetrator​Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
yes
yes (co-administration study)
Comment: administered with cyclosporine: mean Cmax and AUC were increased by 512% and 148%, respectively, relative to administration of sirolimus alone. However, when given 4 hours after cyclosporine administration, sirolimus Cmax and AUC were both increased by only 33% compared with administration of sirolimus alone; administered with diltiazem: Sirolimus Cmax, tmax, and AUC were increased 1.4-, 1.3-, and 1.6-fold, respectively. Sirolimus did not affect the pharmacokinetics of either diltiazem or its metabolites; administered with erythromycin: Sirolimus Cmax and AUC were increased 4.4- and 4.2-fold respectively and tmax was increased by 0.4 hr. Sirolimus did not affect the pharmacokinetics of either diltiazem or its metabolites; administered with ketoconazole; increases in sirolimus Cmax, tmax, and AUC of 4.3-fold, 38%, and 10.9-fold. Single-dose sirolimus did not affect steady-state 12-hour plasma ketoconazole concentrations; administered with rifampin; decreased sirolimus AUC and Cmax by about 82% and 71%, respectively; administered with verapamil: l. Sirolimus Cmax and AUC were increased 2.3- and 2.2-fold, respectively. Cmax and AUC of the pharmacologically active S(-) enantiomer of verapamil were both increased 1.5-fold and tmax was decreased by 1.2 hr;
Page: 19, 27-29
yes
yes (co-administration study)
Comment: administered with cyclosporine: mean Cmax and AUC were increased by 512% and 148%, respectively, relative to administration of sirolimus alone. However, when given 4 hours after cyclosporine administration, sirolimus Cmax and AUC were both increased by only 33% compared with administration of sirolimus alone; administered with diltiazem: Sirolimus Cmax, tmax, and AUC were increased 1.4-, 1.3-, and 1.6-fold, respectively. Sirolimus did not affect the pharmacokinetics of either diltiazem or its metabolites; administered with erythromycin: Sirolimus Cmax and AUC were increased 4.4- and 4.2-fold respectively and tmax was increased by 0.4 hr. Sirolimus did not affect the pharmacokinetics of either diltiazem or its metabolites; administered with ketoconazole; increases in sirolimus Cmax, tmax, and AUC of 4.3-fold, 38%, and 10.9-fold. Single-dose sirolimus did not affect steady-state 12-hour plasma ketoconazole concentrations; administered with rifampin; decreased sirolimus AUC and Cmax by about 82% and 71%, respectively; administered with verapamil: l. Sirolimus Cmax and AUC were increased 2.3- and 2.2-fold, respectively. Cmax and AUC of the pharmacologically active S(-) enantiomer of verapamil were both increased 1.5-fold and tmax was decreased by 1.2 hr;
Page: 19, 27-29
PubMed

PubMed

TitleDatePubMed
Antifungal activities of rapamycin and its derivatives, prolylrapamycin, 32-desmethylrapamycin, and 32-desmethoxyrapamycin.
1998 May
Antifungal rapamycin analogues with reduced immunosuppressive activity.
2000 Jul 3
Rapamycin and less immunosuppressive analogs are toxic to Candida albicans and Cryptococcus neoformans via FKBP12-dependent inhibition of TOR.
2001 Nov
The immunosuppressant rapamycin represses human immunodeficiency virus type 1 replication.
2002 Nov
Rapamycin causes down-regulation of CCR5 and accumulation of anti-HIV beta-chemokines: an approach to suppress R5 strains of HIV-1.
2003 Sep 2
Helicobacter pylori VacA toxin inhibits human immunodeficiency virus infection of primary human T cells.
2006 Dec
In silico prediction of pregnane X receptor activators by machine learning approaches.
2007 Jan
Rapamycin reduces CCR5 density levels on CD4 T cells, and this effect results in potentiation of enfuvirtide (T-20) against R5 strains of human immunodeficiency virus type 1 in vitro.
2007 Jul
Hormonally active vitamin D3 (1alpha,25-dihydroxycholecalciferol) triggers autophagy in human macrophages that inhibits HIV-1 infection.
2011 May 27
Patents

Sample Use Guides

For de novo renal transplant patients, it is recommended that Rapamune (Sirolimus) Oral Solution and Tablets be used initially in a regimen with cyclosporine and corticosteroids. A loading dose of Rapamune equivalent to 3 times the maintenance dose should be given, i.e. a daily maintenance dose of 2 mg should be preceded with a loading dose of 6 mg.
Route of Administration: Oral
Mutant patient cell line with the heterozygous R155H mutation was obtained from the Muscle Tissue Culture Collection. Cells were seeded onto 6-well plates and treated with either 0, 1, 10, or 100 μM concentrations of rapamycin for varying time points either 24 or 48 hours. Rapamycin treatment showed an improvement in the autophagy markers p62/SQSTM1 and LC3-I/II. Targeting the mTOR pathway ameliorates an increasing list of disorders, and these findings suggest that valosin containing protein (VCP) disease and related neurodegenerative multisystem proteinopathies can now be included as disorders that can potentially be ameliorated by rapalogs.
Substance Class Chemical
Created
by admin
on Sat Jun 26 05:06:28 UTC 2021
Edited
by admin
on Sat Jun 26 05:06:28 UTC 2021
Record UNII
W36ZG6FT64
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
SIROLIMUS
EMA EPAR   HSDB   INN   MART.   ORANGE BOOK   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
SIROLIMUS [VANDF]
Common Name English
AY-22989
Code English
SM-88 COMPONENT SIROLIMUS
Code English
WY-090217
Code English
RAPAMYCIN [MI]
Common Name English
SIROLIMUS [JAN]
Common Name English
NSC-226080
Code English
NAB-RAPAMYCIN COMPONENT RAPAMYCIN
Common Name English
SIROLIMUS [HSDB]
Common Name English
RPM
Common Name English
SIROLIMUS [WHO-DD]
Common Name English
L04AA10
Code English
RAPA
Common Name English
SIROLIMUS [INN]
Common Name English
SIROLIMUS [ORANGE BOOK]
Common Name English
NPC-12G
Common Name English
SIROLIMUS [USP-RS]
Common Name English
RAPAMYCIN
MI  
Common Name English
SIROLIMUS [USAN]
Common Name English
RAPAMUNE
Brand Name English
SIROLIMUS [EMA EPAR]
Common Name English
RAPALIMUS
Brand Name English
SIROLIMUS [MART.]
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 434114
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
FDA ORPHAN DRUG 524916
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
FDA ORPHAN DRUG 453114
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
WHO-VATC QL04AA10
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FDA ORPHAN DRUG 568416
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FDA ORPHAN DRUG 327210
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NCI_THESAURUS C261
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FDA ORPHAN DRUG 698619
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FDA ORPHAN DRUG 616217
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FDA ORPHAN DRUG 379312
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NDF-RT N0000175624
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NCI_THESAURUS C574
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FDA ORPHAN DRUG 184304
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EU-Orphan Drug EU/3/17/1910
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
FDA ORPHAN DRUG 237007
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NDF-RT N0000175605
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FDA ORPHAN DRUG 391013
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LIVERTOX 889
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FDA ORPHAN DRUG 540516
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
NDF-RT N0000175550
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
FDA ORPHAN DRUG 678319
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
FDA ORPHAN DRUG 469915
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
FDA ORPHAN DRUG 628918
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
FDA ORPHAN DRUG 508515
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
EMA ASSESSMENT REPORTS RAPAMUNE (AUTHORIZED: GRAFT REJECTION)
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
NDF-RT N0000175625
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
WHO-ATC S01XA23
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
CFR 21 CFR 862.3840
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
EMA ASSESSMENT REPORTS RAPAMUNE (AUTHORIZED: KINDEY TRANSPLANTATION)
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
FDA ORPHAN DRUG 555516
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
WHO-ATC L04AA10
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
Code System Code Type Description
MESH
D020123
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
PRIMARY
MERCK INDEX
M9502
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
PRIMARY Merck Index
IUPHAR
6031
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
PRIMARY
EVMPD
SUB10537MIG
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
PRIMARY
INN
7104
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
PRIMARY
USP_CATALOG
1612765
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
PRIMARY USP-RS
NCI_THESAURUS
C1212
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
PRIMARY
ChEMBL
CHEMBL413
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
PRIMARY
RXCUI
35302
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
PRIMARY RxNorm
HSDB
7284
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
PRIMARY
LACTMED
Sirolimus
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
PRIMARY
PUBCHEM
5284616
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
PRIMARY
FDA UNII
W36ZG6FT64
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
PRIMARY
WIKIPEDIA
SIROLIMUS
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
PRIMARY
DRUG BANK
DB00877
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
PRIMARY
JAPANESE REVIEW
RAPALIMUS
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
PRIMARY APPROVED JULY 2014
DRUG CENTRAL
2446
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
PRIMARY
CAS
53123-88-9
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
PRIMARY
EPA CompTox
53123-88-9
Created by admin on Sat Jun 26 05:06:29 UTC 2021 , Edited by admin on Sat Jun 26 05:06:29 UTC 2021
PRIMARY
Related Record Type Details
METABOLIC ENZYME -> SUBSTRATE
BINDER->LIGAND
Sirolimus is extensively bound (approximately 92%) to human plasma proteins, mainly serum albumin (97%), ?1-acid glycoprotein, and lipoproteins.
BINDING
EXCRETED UNCHANGED
URINE
TARGET -> INHIBITOR
TARGET -> INHIBITOR
TARGET -> INHIBITOR
TARGET -> INHIBITOR
TRANSPORTER -> INHIBITOR
Related Record Type Details
METABOLITE ACTIVE -> PARENT
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC
Tmax PHARMACOKINETIC ORAL ADMINISTRATION