Compounds > voclosporin
Page last updated: 2024-12-11

voclosporin

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Description

voclosporin: semi-synthetic cyclosporine A analog & calcineurin inhibitor; FDA approved use to treat lupus nephritis. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6918486
CHEBI ID135957
SCHEMBL ID12632344
MeSH IDM0527077

Synonyms (62)

Synonym
voclosporin
isatx-247
isa-247
lx-211
voclera
luveniq
r-1524
trans-isa-247
lx-214
CHEBI:135957
isatx 247
D09033
voclosporin (usan/inn)
515814-01-4
(3s,6s,9s,12r,15s,18s,21s,24s,30s,33s)-30-ethyl-33-[(1r,2r,4e)-1-hydroxy-2-methylhepta-4,6-dienyl]-1,4,7,10,12,15,19,25,28-nonamethyl-6,9,18,24-tetrakis(2-methylpropyl)-3,21-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacontane-2,5,8,1
voclosporin [usan:inn]
lupkynis
trans-isa 247
isatx247
lx211
isa247
2pn063x6b1 ,
isa(tx)247
unii-2pn063x6b1
r 1524
515814-00-3
isa 247
cyclosporin a, 6-((2s,3r,4r)-3-hydroxy-4-methyl-2-(methylamino)-6,8-nonadienoic acid)-
voclosporin [mi]
cyclo(l-alanyl-d-alanyl-n-methyl-l-leucyl-n-methyl-l-leucyl-n-methyl-l-valyl- ((2s,3r,4r,6e)-3-hydroxy-4-methyl-2-(methylamino)nona-6,8-dienoyl)-(2s)-2- aminobutanoyl-n-methylglycyl-n-methyl-l-leucyl-l-valyl-n-methyl-l-leucyl)
voclosporin [orange book]
voclosporin [who-dd]
voclosporin [inn]
voclosporin [usan]
cyclosporin a, 6-((2s,3r,4r,6e)-3-hydroxy-4-methyl-2-(methylamino)-6,8- nonadienoic acid)-
cyclo (((e,z)-(2s,3r,4r)-3-hydroxy-4-methyl-2-(methylamino)nona-6,8-dienoyl)-l-2-aminobytyrl-n-methyl-glycyl-n-methyl-l-leucyl-l-valyl-n-methyl-l-leucyl-l-alanyl-d-alanyl-n-methyl-l-leucyl-n-methyl-l-leucyl-n-methyl-l-valyl)
voclosporin [mart.]
6-[(2s,3r,4r,6e)-3-hydroxy-4-methyl-2-(methylamino)-6,8-nonadienoic acid]cyclosporin a
R1524 ,
3ODI
SCHEMBL12632344
CS-0026210
HY-106638
DB11693
(3s,6s,9s,12r,15s,18s,21s,24s,30s,33s)-30-ethyl-33-((1r,2r,e)-1-hydroxy-2-methylhepta-4,6-dien-1-yl)-6,9,18,24-tetraisobutyl-3,21-diisopropyl-1,4,7,10,12,15,19,25,28-nonamethyl-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2,5,8,11,14,17,20,23
voclosporine
Q7939256
isatx-247; luveniq
AT27977
MS-32055
1,11-anhydro[l-alanyl-d-alanyl-n-methyl-l-leucyl-n-methyl-l-leucyl- n-methyl-l-valyl-[(2s,3r,4r,6e)-3-hydroxy-4-methyl- 2-(methylamino)nona-6,8-dienoyl][(2s)-2-aminobutanoyl]- n-methylglycyl-n-methyl-l-leucyl-l-valyl-n-methyl-l-leucine]
gtpl11388
e-isa247
EX-A5922
(3s,6s,9s,12r,15s,18s,21s,24s,30s,33s)-30-ethyl-33-[(1r,2r,4e)-1-hydroxy-2-methylhepta-4,6-dien-1-yl]-1,4,7,10,12,15,19,25,28-nonamethyl-6,9,18,24-tetrakis(2-methylpropyl)-3,21-bis(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2,5
DTXSID401030488
voclosporina
voclosporinum
cyclo(l-alanyl-d-alanyl-n-methyl-l-leucyl-n-methyl-l-leucyl-n-methyl-l-valyl-((2s,3r,4r,6e)-3-hydroxy-4-methyl-2-(methylamino)nona-6,8-dienoyl)-(2s)-2-aminobutanoyl-n-methylglycyl-n-methyl-l-leucyl-l-valyl-n-methyl-l-leucyl)
1,11-anhydro(l-alanyl-d-alanyl-n-methyl-l-leucyl-n-methyl-l-leucyl- n-methyl-l-valyl-((2s,3r,4r,6e)-3-hydroxy-4-methyl- 2-(methylamino)nona-6,8-dienoyl)((2s)-2-aminobutanoyl)- n-methylglycyl-n-methyl-l-leucyl-l-valyl-n-methyl-l-leucine)
voclosporin (mart.)
AKOS040742818

Research Excerpts

Overview

Voclosporin (VCS) is a novel calcineurin (CN) inhibitor intended for prevention of organ graft rejection and treatment of lupus nephritis.

ExcerptReferenceRelevance
"Voclosporin is a CNI with a consistent pharmacokinetic-pharmacodynamic relationship resulting from enhanced calcineurin binding and reduced drug and metabolite load. "( Voclosporin: a novel calcineurin inhibitor for the treatment of lupus nephritis.
Engelke, K; Huizinga, RB; Lerma, E; van Gelder, T, 2022)		3.61
"Voclosporin (VCS) is a novel calcineurin (CN) inhibitor intended for prevention of organ graft rejection and treatment of lupus nephritis. "( Voclosporin food effect and single oral ascending dose pharmacokinetic and pharmacodynamic studies in healthy human subjects.
Aspeslet, LJ; Foster, RT; Freitag, DG; Huizinga, RB; Ling, SY; Mayo, PR, 2013)		3.28
"Voclosporin is a novel calcineurin inhibitor intended for prevention of organ graft rejection and treatment of lupus nephritis. "( Pharmacokinetics of voclosporin in renal impairment and hepatic impairment.
Aspeslet, LJ; Foster, RT; Freitag, DG; Huizinga, RB; Ling, SY; Mayo, PR, 2013)		2.16
"Voclosporin is a novel calcineurin inhibitor intended for prevention of organ graft rejection and treatment of lupus nephritis. "( Cytochrome P450 3A and P-glycoprotein drug-drug interactions with voclosporin.
Aspeslet, LJ; Foster, RT; Freitag, DG; Huizinga, RB; Larouche, R; Ling, SY; Mayo, PR, 2014)		2.08
"Voclosporin (VCS, ISA247) is a novel calcineurin inhibitor being developed for organ transplantation. "( The PROMISE study: a phase 2b multicenter study of voclosporin (ISA247) versus tacrolimus in de novo kidney transplantation.
Busque, S; Cantarovich, M; Gaber, AO; Gaston, R; Huizinga, RB; Ling, S; Mayo, PR; Meier-Kriesche, HU; Mulgaonkar, S, 2011)		2.06

Toxicity

Voclosporin (VOC), a novel CNI, no longer requires drug level monitoring and seems to lack these adverse effects. hypertension and drug-drug interactions still occur.

ExcerptReferenceRelevance
" There were more serious adverse events in both voclosporin groups, and more deaths in the low-dose group compared to placebo and high-dose voclosporin groups (11."( A randomized, controlled double-blind study comparing the efficacy and safety of dose-ranging voclosporin with placebo in achieving remission in patients with active lupus nephritis.
Dooley, MA; Huizinga, RB; Lysenko, L; Navarra, SV; Pendergraft, WF; Romero-Diaz, J; Rovin, BH; Solomons, N; Tumlin, J, 2019)		0.99
" The adverse event profile was balanced between the two groups; serious adverse events occurred in 37 (21%) of 178 in the voclosporin group and 38 (21%) of 178 patients in the placebo group."( Efficacy and safety of voclosporin versus placebo for lupus nephritis (AURORA 1): a double-blind, randomised, multicentre, placebo-controlled, phase 3 trial.
Arriens, C; Caster, DJ; Gibson, K; Ginzler, EM; Huizinga, RB; Kaplan, J; Lisk, L; Navarra, S; Parikh, SV; Randhawa, S; Romero-Diaz, J; Rovin, BH; Solomons, N; Teng, YKO, 2021)		1.14
" However, tacrolimus + MMF did pose a greater risk of serious adverse events than monotherapy."( A network meta-analysis of randomized controlled trials comparing the effectiveness and safety of voclosporin or tacrolimus plus mycophenolate mofetil as induction treatment for lupus nephritis.
Lee, YH; Song, GG, 2023)		1.13
" The incidence of adverse events (AEs) was similar (91."( Update on the Efficacy and Safety Profile of Voclosporin: An Integrated Analysis of Clinical Trials in Lupus Nephritis.
Arriens, C; Askanase, AD; Atsumi, T; Caster, DJ; Gibson, K; Ginzler, EM; Gluck, R; Huizinga, RB; Lisk, L; Parikh, SV; Randhawa, S; Saxena, A; Solomons, N; Teng, YKO, 2023)		1.17
" Voclosporin (VOC), a novel CNI, no longer requires drug level monitoring and seems to lack these adverse effects, although hypertension and drug-drug interactions still occur."( Voclosporin: Unique Chemistry, Pharmacology and Toxicity Profile, and Possible Options for Implementation into the Management of Lupus Nephritis.
Anders, HJ; Gaikwad, AB; Kale, A; Lei, Y; Shelke, V, 2023)		3.26

Pharmacokinetics

ExcerptReferenceRelevance
" Geometric mean ratios (renal/hepatic impairment-to-normal) and 90% confidence intervals for Cmax and AUC were calculated."( Pharmacokinetics of voclosporin in renal impairment and hepatic impairment.
Aspeslet, LJ; Foster, RT; Freitag, DG; Huizinga, RB; Ling, SY; Mayo, PR, 2013)		0.71

Compound-Compound Interactions

ExcerptReferenceRelevance
" Drug-drug interactions involving voclosporin and CYP3A substrates are not expected."( Cytochrome P450 3A and P-glycoprotein drug-drug interactions with voclosporin.
Aspeslet, LJ; Foster, RT; Freitag, DG; Huizinga, RB; Larouche, R; Ling, SY; Mayo, PR, 2014)		0.92

Dosage Studied

An open-label phase 1 study was conducted to evaluate the effect of voclosporin following dosing with mycophenolate mofetil in subjects with systemic lupus erythematosus (SLE)

ExcerptRelevanceReference
" Both groups were dosed twice daily to maintain a 12-hour drug-trough level of 150 ng/mL."( Compared with cyclosporine, ISATX247 significantly prolongs renal-allograft survival in a nonhuman primate model.
Bernsteen, L; Borie, DC; Brignolo, L; Christe, KL; Gregory, CR; Griffey, SM; Hubble, RW; Kyles, AE; Morris, RE; Paniagua, RT; Spinner, A; Tarantal, AF; Wagner, GS, 2004)		0.32
" The strong correlation between ISA247 concentrations and efficacy might allow for accurate dosing of patients compared with existing calcineurin inhibitors."( Efficacy of ISA247 in plaque psoriasis: a randomised, multicentre, double-blind, placebo-controlled phase III study.
Bissonnette, R; Huizinga, RB; Lynde, CW; Maksymowych, WP; Papp, K; Rosoph, L; Searles, G; Shear, NH; Wasel, N, 2008)		0.35
"The aims of this population-pharmacokinetic/pharmacodynamic (POP-PKPD) analysis of voclosporin in renal allograft patients were to build a POP-PKPD model for voclosporin and calcineurin activity (CNa) and identify clinically relevant covariates that could assist dosing of the drug."( Population PKPD of voclosporin in renal allograft patients.
Aspeslet, LJ; Foster, RT; Freitag, DG; Huizinga, RB; Ling, SY; Mayo, PR, 2014)		0.96
"An open-label phase 1 study was conducted to evaluate the effect of voclosporin following dosing with mycophenolate mofetil (MMF) on blood levels of mycophenolic acid (MPA, the active moiety of MMF) and MPA glucuronide (MPAG, the pharmacologically inactive metabolite of MMF) in subjects with systemic lupus erythematosus (SLE) and to assess the safety and tolerability of the combination."( Voclosporin: a novel calcineurin inhibitor with no impact on mycophenolic acid levels in patients with SLE.
Huizinga, RB; Lisk, L; Solomons, N; van Gelder, T, 2022)		2.4
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
homodetic cyclic peptideA homodetic cyclic peptide is a cyclic peptide in which the ring consists solely of amino-acid residues in peptide linkages.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (2)

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Cyclophilin AHomo sapiens (human)Kd0.01500.01500.01500.0150AID977611
Chain A, Cyclophilin AHomo sapiens (human)Kd0.01500.01500.01500.0150AID977611
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (1)

Assay IDTitleYearJournalArticle
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2011Acta crystallographica. Section D, Biological crystallography, Feb, Volume: 67, Issue:Pt 2
Structural basis for the cyclophilin A binding affinity and immunosuppressive potency of E-ISA247 (voclosporin).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (53)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's13 (24.53)29.6817
2010's17 (32.08)24.3611
2020's23 (43.40)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 62.49

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index62.49 (24.57)
Research Supply Index4.28 (2.92)
Research Growth Index4.88 (4.65)
Search Engine Demand Index102.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (62.49)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials15 (26.79%)5.53%
Reviews16 (28.57%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other25 (44.64%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
verapamil
Verapamil: A calcium channel blocker that is a class IV anti-arrhythmia agent.. verapamil : A racemate comprising equimolar amounts of dexverapamil and (S)-verapamil. An L-type calcium channel blocker of the phenylalkylamine class, it is used (particularly as the hydrochloride salt) in the treatment of hypertension, angina pectoris and cardiac arrhythmia, and as a preventive medication for migraine.. 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile : A tertiary amino compound that is 3,4-dimethoxyphenylethylamine in which the hydrogens attached to the nitrogen are replaced by a methyl group and a 4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl group.		6.833aromatic ether;
nitrile;
polyether;
tertiary amino compound
ketoconazole
1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively.		6.833dichlorobenzene;
dioxolane;
ether;
imidazoles;
N-acylpiperazine;
N-arylpiperazine
midazolam
Midazolam: A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH.. midazolam : An imidazobenzodiazepine that is 4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted by a methyl, 2-fluorophenyl and chloro groups at positions 1, 6 and 8, respectively.		6.833imidazobenzodiazepine;
monofluorobenzenes;
organochlorine compound		anticonvulsant;
antineoplastic agent;
anxiolytic drug;
apoptosis inducer;
central nervous system depressant;
GABAA receptor agonist;
general anaesthetic;
muscle relaxant;
sedative
tazarotene
tazarotene: a topical acetylenic retinoid; a topical kerytolytic. tazarotene : The ethyl ester of tazarotenic acid. A prodrug for tazarotenic acid, it is used for the treatment of psoriasis, acne, and sun-damaged skin.		3.1210acetylenic compound;
ethyl ester;
pyridines;
retinoid;
thiochromane		keratolytic drug;
prodrug;
teratogenic agent
pyrroles
1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.		3.1510pyrrole;
secondary amine
quinazolines
Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.		3.1510azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinazolines
ribavirin
Rebetron: Rebetron is tradename		2.15101-ribosyltriazole;
aromatic amide;
monocarboxylic acid amide;
primary carboxamide		anticoronaviral agent;
antiinfective agent;
antimetabolite;
antiviral agent;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
bortezomib
[no description available]		3.4110amino acid amide;
L-phenylalanine derivative;
pyrazines		antineoplastic agent;
antiprotozoal drug;
protease inhibitor;
proteasome inhibitor
fumaric acid
fumaric acid: see also record for ferrous fumarate; use FUMARATES for general fumaric acid esters. fumaric acid : A butenedioic acid in which the C=C double bond has E geometry. It is an intermediate metabolite in the citric acid cycle.		3.1210butenedioic acidfood acidity regulator;
fundamental metabolite;
geroprotector
tacrolimus
Tacrolimus: A macrolide isolated from the culture broth of a strain of Streptomyces tsukubaensis that has strong immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro.. tacrolimus (anhydrous) : A macrolide lactam containing a 23-membered lactone ring, originally isolated from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis.		10.76115macrolide lactambacterial metabolite;
immunosuppressive agent
mycophenolic acid
Mycophenolic Acid: Compound derived from Penicillium stoloniferum and related species. It blocks de novo biosynthesis of purine nucleotides by inhibition of the enzyme inosine monophosphate dehydrogenase (IMP DEHYDROGENASE). Mycophenolic acid exerts selective effects on the immune system in which it prevents the proliferation of T-CELLS, LYMPHOCYTES, and the formation of antibodies from B-CELLS. It may also inhibit recruitment of LEUKOCYTES to sites of INFLAMMATION.. mycophenolate : A monocarboxylic acid anion resulting from the removal of a proton from the carboxy group of mycophenolic acid.. mycophenolic acid : A member of the class of 2-benzofurans that is 2-benzofuran-1(3H)-one which is substituted at positions 4, 5, 6, and 7 by methyl, methoxy, (2E)-5-carboxy-3-methylpent-2-en-1-yl, and hydroxy groups, respectively. It is an antibiotic produced by Penicillium brevi-compactum, P. stoloniferum, P. echinulatum and related species. An immunosuppressant, it is widely used (partiularly as its sodium salt and as the 2-(morpholin-4-yl)ethyl ester prodrug, mycophenolate mofetil) to prevent tissue rejection following organ transplants and for the treatment of certain autoimmune diseases.		13.62832-benzofurans;
gamma-lactone;
monocarboxylic acid;
phenols		anticoronaviral agent;
antimicrobial agent;
antineoplastic agent;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
environmental contaminant;
immunosuppressive agent;
mycotoxin;
Penicillium metabolite;
xenobiotic
digoxin
Digoxin: A cardiotonic glycoside obtained mainly from Digitalis lanata; it consists of three sugars and the aglycone DIGOXIGENIN. Digoxin has positive inotropic and negative chronotropic activity. It is used to control ventricular rate in ATRIAL FIBRILLATION and in the management of congestive heart failure with atrial fibrillation. Its use in congestive heart failure and sinus rhythm is less certain. The margin between toxic and therapeutic doses is small. (From Martindale, The Extra Pharmacopoeia, 30th ed, p666). digoxin : A cardenolide glycoside that is digitoxin beta-hydroxylated at C-12. A cardiac glycoside extracted from the foxglove plant, Digitalis lanata, it is used to control ventricular rate in atrial fibrillation and in the management of congestive heart failure with atrial fibrillation, but the margin between toxic and therapeutic doses is small.		6.833cardenolide glycoside;
steroid saponin		anti-arrhythmia drug;
cardiotonic drug;
EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor;
epitope
sirolimus
Sirolimus: A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.. sirolimus : A macrolide lactam isolated from Streptomyces hygroscopicus consisting of a 29-membered ring containing 4 trans double bonds, three of which are conjugated. It is an antibiotic, immunosupressive and antineoplastic agent.		3.1510antibiotic antifungal drug;
cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
organic heterotricyclic compound;
secondary alcohol		antibacterial drug;
anticoronaviral agent;
antineoplastic agent;
bacterial metabolite;
geroprotector;
immunosuppressive agent;
mTOR inhibitor
fumarates
Fumarates: Compounds based on fumaric acid.. fumarate(2-) : A C4-dicarboxylate that is the E-isomer of but-2-enedioate(2-)		3.1210butenedioate;
C4-dicarboxylate		human metabolite;
metabolite;
Saccharomyces cerevisiae metabolite
everolimus
[no description available]		3.1510cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
primary alcohol;
secondary alcohol		anticoronaviral agent;
antineoplastic agent;
geroprotector;
immunosuppressive agent;
mTOR inhibitor
tofacitinib
tofacitinib : A pyrrolopyrimidine that is pyrrolo[2,3-d]pyrimidine substituted at position 4 by an N-methyl,N-(1-cyanoacetyl-4-methylpiperidin-3-yl)amino moiety. Used as its citrate salt to treat moderately to severely active rheumatoid arthritis.		3.1510N-acylpiperidine;
nitrile;
pyrrolopyrimidine;
tertiary amino compound		antirheumatic drug;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
sotrastaurin
sotrastaurin: a potent protein kinase C-selective inhibitor; structure in first source. sotrastaurin : A member of the class of maleimides that is maleimide which is substituted at position 3 by an indol-3-yl group and at position 4 by a quinazolin-4-yl group, which in turn is substituted at position 2 by a 4-methylpiperazin-1-yl group. It is a potent and selective inhibitor of protein kinase C and has been investigated as an immunosuppresant in renal transplant patients.		3.1510indoles;
maleimides;
N-alkylpiperazine;
N-arylpiperazine;
quinazolines		anticoronaviral agent;
EC 2.7.11.13 (protein kinase C) inhibitor;
immunosuppressive agent
piperidines
Piperidines: A family of hexahydropyridines.		3.1510
cyclosporine
Cyclosporine: A cyclic undecapeptide from an extract of soil fungi. It is a powerful immunosupressant with a specific action on T-lymphocytes. It is used for the prophylaxis of graft rejection in organ and tissue transplantation. (From Martindale, The Extra Pharmacopoeia, 30th ed).		17.086823
ConditionIndicatedRelationship StrengthStudiesTrials
Glomerulonephritis, Lupus
[description not available]		010.53223
Lupus Nephritis
Glomerulonephritis associated with autoimmune disease SYSTEMIC LUPUS ERYTHEMATOSUS. Lupus nephritis is histologically classified into 6 classes: class I - normal glomeruli, class II - pure mesangial alterations, class III - focal segmental glomerulonephritis, class IV - diffuse glomerulonephritis, class V - diffuse membranous glomerulonephritis, and class VI - advanced sclerosing glomerulonephritis (The World Health Organization classification 1982).		010.53223
Libman-Sacks Disease
[description not available]		06.4541
Lupus Erythematosus, Systemic
A chronic, relapsing, inflammatory, and often febrile multisystemic disorder of connective tissue, characterized principally by involvement of the skin, joints, kidneys, and serosal membranes. It is of unknown etiology, but is thought to represent a failure of the regulatory mechanisms of the autoimmune system. The disease is marked by a wide range of system dysfunctions, an elevated erythrocyte sedimentation rate, and the formation of LE cells in the blood or bone marrow.		06.4541
Kidney Failure
A severe irreversible decline in the ability of kidneys to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism.		09.81109
Renal Insufficiency
Conditions in which the KIDNEYS perform below the normal level in the ability to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism. Renal insufficiency can be classified by the degree of kidney damage (as measured by the level of PROTEINURIA) and reduction in GLOMERULAR FILTRATION RATE.		09.81109
2019 Novel Coronavirus Disease
[description not available]		03.2310
Caliciviridae Infections
Virus diseases caused by CALICIVIRIDAE. They include HEPATITIS E; VESICULAR EXANTHEMA OF SWINE; acute respiratory infections in felines, rabbit hemorrhagic disease, and some cases of gastroenteritis in humans.		02.1510
Liver Dysfunction
[description not available]		09.799
Liver Diseases
Pathological processes of the LIVER.		09.799
Palmoplantaris Pustulosis
[description not available]		011.22138
Psoriasis
A common genetically determined, chronic, inflammatory skin disease characterized by rounded erythematous, dry, scaling patches. The lesions have a predilection for nails, scalp, genitalia, extensor surfaces, and the lumbosacral region. Accelerated epidermopoiesis is considered to be the fundamental pathologic feature in psoriasis.		016.22138
Autoimmune Disease
[description not available]		02.0510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.0510
Neuroretinitis
[description not available]		02.0510
Autoimmune Diseases
Disorders that are characterized by the production of antibodies that react with host tissues or immune effector cells that are autoreactive to endogenous peptides.		02.0510
Retinitis
Inflammation of the RETINA. It is rarely limited to the retina, but is commonly associated with diseases of the choroid (CHORIORETINITIS) and of the OPTIC DISK (neuroretinitis).		02.0510
Uveitis
Inflammation of part or all of the uvea, the middle (vascular) tunic of the eye, and commonly involving the other tunics (sclera and cornea, and the retina). (Dorland, 27th ed)		02.4620
Complications of Diabetes Mellitus
[description not available]		012.612525
Blood Pressure, High
[description not available]		012.612525
Chronic Kidney Failure
[description not available]		012.612525
Complication, Postoperative
[description not available]		012.612525
Cardiovascular Diseases
Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.		012.612525
Hypertension
Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.		012.612525
Kidney Failure, Chronic
The end-stage of CHRONIC RENAL INSUFFICIENCY. It is characterized by the severe irreversible kidney damage (as measured by the level of PROTEINURIA) and the reduction in GLOMERULAR FILTRATION RATE to less than 15 ml per min (Kidney Foundation: Kidney Disease Outcome Quality Initiative, 2002). These patients generally require HEMODIALYSIS or KIDNEY TRANSPLANTATION.		012.612525
Postoperative Complications
Pathologic processes that affect patients after a surgical procedure. They may or may not be related to the disease for which the surgery was done, and they may or may not be direct results of the surgery.		012.612525
Adjuvant Arthritis
[description not available]		02.9310
Autoimmune Diabetes
[description not available]		02.9310
Diabetes Mellitus, Type 1
A subtype of DIABETES MELLITUS that is characterized by INSULIN deficiency. It is manifested by the sudden onset of severe HYPERGLYCEMIA, rapid progression to DIABETIC KETOACIDOSIS, and DEATH unless treated with insulin. The disease may occur at any age, but is most common in childhood or adolescence.		02.9310
Dermatoses
[description not available]		02.9510
Skin Diseases
Diseases involving the DERMIS or EPIDERMIS.		02.9510
Eye Disorders
[description not available]		02.9510
Eye Diseases
Diseases affecting the eye.		02.9510
Adverse Drug Event
[description not available]		03.4311
Drug-Related Side Effects and Adverse Reactions
Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals.		03.4311