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ciclosporin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
ciclosporin derivatives	760	59865-13-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: neoral ciclosporin cyclosporine cyclosporin ciclosporine cyclosporin A	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). Molecular weight: 1202.64 Formula: C62H111N11O12 CLOGP: 12 LIPINSKI: 3 HAC: 23 HDO: 5 TPSA: 278.80 ALOGS: -5.10 ROTB: 15 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

neoral
ciclosporin
cyclosporine
cyclosporin
ciclosporine
cyclosporin A

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).

Molecular weight: 1202.64
Formula: C62H111N11O12
CLOGP: 12
LIPINSKI: 3
HAC: 23
HDO: 5
TPSA: 278.80
ALOGS: -5.10
ROTB: 15

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.25	g	O
0.25	g	P

ADMET properties:

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Property	Value	Reference
CL (Clearance)	7.50 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	7.30 hours	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	30 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	3.30 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.66 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
EoM (Fraction excreted unchanged in urine)	0.10 %	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.07 %	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.01 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

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Date	Agency	Company
Feb. 21, 2020	PMDA	Novartis Pharma K.K.
May 19, 2015	EMA	Santen Oy
Nov. 14, 1983	FDA	NOVARTIS

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FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Cytomegalovirus infection	1647.08	9.61	868	153356	20084	63314714
Eye irritation	1527.78	9.61	839	153385	21132	63313666
Transplant dysfunction	1490.07	9.61	528	153696	4344	63330454
Transplant rejection	1426.60	9.61	638	153586	10142	63324656
Graft versus host disease	1003.93	9.61	434	153790	6329	63328469
Acute graft versus host disease	904.45	9.61	357	153867	4071	63330727
Product use in unapproved indication	820.51	9.61	1520	152704	177560	63157238
Chronic graft versus host disease	791.02	9.61	294	153930	2808	63331990
Acute graft versus host disease in skin	717.98	9.61	282	153942	3170	63331628
Ovarian cyst	690.48	9.61	449	153775	15496	63319302

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Cytomegalovirus infection	1891.94	10.79	1164	121296	24971	34809500
Graft versus host disease	1274.07	10.79	658	121802	9911	34824560
Acute graft versus host disease	1052.61	10.79	495	121965	6008	34828463
Acute graft versus host disease in skin	1037.76	10.79	458	122002	4743	34829728
Product use in unapproved indication	954.34	10.79	1574	120886	115925	34718546
Chronic graft versus host disease	947.07	10.79	408	122052	3965	34830506
Epstein-Barr virus infection	778.17	10.79	425	122035	7203	34827268
Post transplant lymphoproliferative disorder	731.10	10.79	387	122073	6141	34828330
Graft versus host disease in gastrointestinal tract	711.16	10.79	317	122143	3366	34831105
Kidney transplant rejection	654.12	10.79	377	122083	7120	34827351

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Cytomegalovirus infection	3300.47	9.78	1868	233854	40776	79467890
Graft versus host disease	2179.23	9.78	1006	234716	14020	79494646
Acute graft versus host disease	1992.34	9.78	841	234881	9326	79499340
Product use in unapproved indication	1816.17	9.78	2904	232818	247455	79261211
Acute graft versus host disease in skin	1681.14	9.78	687	235035	6971	79501695
Chronic graft versus host disease	1646.19	9.78	654	235068	6127	79502539
Transplant rejection	1635.21	9.78	900	234822	18537	79490129
Transplant dysfunction	1480.72	9.78	617	235105	6604	79502062
Epstein-Barr virus infection	1401.70	9.78	735	234987	13681	79494985
Post transplant lymphoproliferative disorder	1391.13	9.78	679	235043	10785	79497881

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L04AD01	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS IMMUNOSUPPRESSANTS IMMUNOSUPPRESSANTS Calcineurin inhibitors
ATC	S01XA18	SENSORY ORGANS OPHTHALMOLOGICALS OTHER OPHTHALMOLOGICALS Other ophthalmologicals
CHEBI has role	CHEBI:25212	metabolites
CHEBI has role	CHEBI:35705	immunosuppressive agents
CHEBI has role	CHEBI:35718	antifungal agents
CHEBI has role	CHEBI:35842	anti-rheumatic drugs
CHEBI has role	CHEBI:37153	protein serine/threonine phosphatase inhibitors
CHEBI has role	CHEBI:49167	anti-asthmatic drugs
CHEBI has role	CHEBI:50177	dermatologic agent
CHEBI has role	CHEBI:50903	carcinogen

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Tear film insufficiency	indication	46152009
Rheumatoid arthritis	indication	69896004	DOID:7148
Kawasaki's disease	indication	75053002	DOID:13378
Keratoconjunctivitis sicca	indication	302896008	DOID:12895
Prevention of Liver Transplant Rejection	indication
Prevention of Cardiac Transplant Rejection	indication
Prevention of Kidney Transplant Rejection	indication
Severe Recalcitrant Psoriasis	indication
Graft-versus-host disease	off-label use	234646005
Pure Red Cell Aplasia associated with Chronic Lymphocytic Leukemia	off-label use

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🐶 Veterinary Drug Use

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Species	Use	Relation
Cats	Allergic dermatitis as manifested by excoriations (including facial and neck), miliary dermatitis, eosinophilic plaques, and self-induced alopecia	Indication
Dogs	Chronic keratoconjunctivitis sicca (KCS)	Indication
Dogs	Chronic superficial keratitis (CSK)	Indication
Dogs	Pruritus associated with allergic dermatitis	Indication
Dogs	Atopic dermatitis	Indication

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🐶 Veterinary products

Product	Applicant	Ingredients
Atopica for Cats	Elanco US Inc.	2

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
0.05%	RESTASIS MULTIDOSE	ABBVIE	N050790	Oct. 27, 2016	RX	EMULSION	OPHTHALMIC	8633162	Aug. 27, 2024	INCREASE TEAR PRODUCTION TO TREAT PATIENTS WITH KERATOCONJUNCTIVITIS SICCA (DRY EYE).
0.05%	RESTASIS MULTIDOSE	ABBVIE	N050790	Oct. 27, 2016	RX	EMULSION	OPHTHALMIC	8648048	Aug. 27, 2024	INCREASE TEAR PRODUCTION IN PATIENTS WITH KERATOCONJUNCTIVITIS SICCA (DRY EYE).
0.05%	RESTASIS MULTIDOSE	ABBVIE	N050790	Oct. 27, 2016	RX	EMULSION	OPHTHALMIC	9248191	Aug. 27, 2024	INCREASE TEAR PRODUCTION TO TREAT PATIENTS WITH KERATOCONJUNCTIVITIS SICCA (DRY EYE).
0.09%	CEQUA	SUN PHARM	N210913	Aug. 14, 2018	RX	SOLUTION	OPHTHALMIC	8980839	Aug. 23, 2033	INCREASE TEAR PRODUCTION IN PATIENTS WITH KERATOCONJUNCTIVITIS SICCA (DRY EYE).
0.09%	CEQUA	SUN PHARM	N210913	Aug. 14, 2018	RX	SOLUTION	OPHTHALMIC	9937225	Aug. 23, 2033	INCREASE TEAR PRODUCTION IN PATIENTS WITH KERATOCONJUNCTIVITIS SICCA (DRY EYE).
0.1%	VERKAZIA	SANTEN	N214965	June 23, 2021	RX	EMULSION	OPHTHALMIC	11612658	Jan. 27, 2026	FOR THE TREATMENT OF VERNAL KERATOCONJUNCTIVITIS IN CHILDREN AND ADULTS
0.1%	VEVYE	NOVALIQ GMBH	N217469	May 30, 2023	RX	SOLUTION	OPHTHALMIC	11154513	Nov. 20, 2038	TREATMENT OF THE SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED)
0.1%	VEVYE	NOVALIQ GMBH	N217469	May 30, 2023	RX	SOLUTION	OPHTHALMIC	11413323	Oct. 11, 2039	TREATMENT OF DRY EYE DISEASE (DED)

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
0.1%	VERKAZIA	SANTEN	N214965	June 23, 2021	RX	EMULSION	OPHTHALMIC	June 23, 2024	NEW PRODUCT
0.1%	VEVYE	NOVALIQ GMBH	N217469	May 30, 2023	RX	SOLUTION	OPHTHALMIC	May 30, 2026	NEW PRODUCT
0.1%	VERKAZIA	SANTEN	N214965	June 23, 2021	RX	EMULSION	OPHTHALMIC	June 23, 2028	FOR THE TREATMENT OF VERNAL KERATOCONJUNCTIVITIS (VKC) IN CHILDREN AND ADULTS

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Peptidyl-prolyl cis-trans isomerase A	Enzyme	P62937	PPIA_HUMAN	MODULATOR	IC50	8.05	WOMBAT-PK	CHEMBL
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN		EC50	6.30	WOMBAT-PK
Canalicular multispecific organic anion transporter 1	Transporter	Q92887	MRP2_HUMAN		IC50	4.87	CHEMBL
Peptidyl-prolyl cis-trans isomerase FKBP1A	Enzyme	P62942	FKB1A_HUMAN		IC50	7.80	WOMBAT-PK
Dihydroorotate dehydrogenase (quinone), mitochondrial	Enzyme	Q02127	PYRD_HUMAN		IC50	6.70	WOMBAT-PK
Multidrug resistance-associated protein 1	Transporter	P33527	MRP1_HUMAN		IC50	5.57	CHEMBL
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN		IC50	4.20	CHEMBL
Canalicular multispecific organic anion transporter 2	Transporter	O15438	MRP3_HUMAN		IC50	6.20	CHEMBL
fMet-Leu-Phe receptor	GPCR	P21462	FPR1_HUMAN	ANTAGONIST	EC50	6.30	IUPHAR
Bile salt export pump	Transporter	O95342	ABCBB_HUMAN		IC50	6.30	CHEMBL

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External reference:

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ID	Source
003420	NDDF
1024	IUPHAR_LIGAND_ID
202817	RXNORM
26496N541O	UNII
3027	MMSL
31626	MMSL
387467008	SNOMEDCT_US
4018761	VUID
4018761	VANDF
4521	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Gengraf	HUMAN PRESCRIPTION DRUG LABEL	1	0074-0541	CAPSULE	50 mg	ORAL	ANDA	26 sections
Gengraf	HUMAN PRESCRIPTION DRUG LABEL	1	0074-0541	CAPSULE	50 mg	ORAL	ANDA	26 sections
Gengraf	HUMAN PRESCRIPTION DRUG LABEL	1	0074-3108	CAPSULE	25 mg	ORAL	ANDA	26 sections
Gengraf	HUMAN PRESCRIPTION DRUG LABEL	1	0074-3108	CAPSULE	25 mg	ORAL	ANDA	26 sections
Gengraf	HUMAN PRESCRIPTION DRUG LABEL	1	0074-3109	CAPSULE	100 mg	ORAL	ANDA	26 sections
Gengraf	HUMAN PRESCRIPTION DRUG LABEL	1	0074-3109	CAPSULE	100 mg	ORAL	ANDA	26 sections
Gengraf	HUMAN PRESCRIPTION DRUG LABEL	1	0074-6463	CAPSULE	25 mg	ORAL	ANDA	26 sections
Gengraf	HUMAN PRESCRIPTION DRUG LABEL	1	0074-6463	CAPSULE	25 mg	ORAL	ANDA	26 sections
Gengraf	HUMAN PRESCRIPTION DRUG LABEL	1	0074-6479	CAPSULE	100 mg	ORAL	ANDA	26 sections
Gengraf	HUMAN PRESCRIPTION DRUG LABEL	1	0074-6479	CAPSULE	100 mg	ORAL	ANDA	26 sections

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