pimecrolimus

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.62 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	0 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Property	Description	Value	Unit	Confidence	Similarity
kinase-safety-class	ACVR2B,CAMK2D,CDK5,EIF2AK3,ERBB2,GRK2,ITK,NTRK2,PDK1,PDK2,PDK4,PRKDC,TEK	13
kinase-selectivity-class	GRK2	1
mdck-mdr1-bcrp-efflux	MDCK-MDR1-BCRP efflux ratio	1.021		High	0.83
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
rat-kpuu-brain	Rat brain Kpuu	0.394	%	High	0.83

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
Dermatitis atopic	472.53	26.30	127	4344	23345	90600631
Eczema	166.72	26.30	71	4400	52799	90571177
Drug ineffective	162.89	26.30	262	4209	1384036	89239940
Dry skin	149.30	26.30	77	4394	87996	90535980
Pruritus	140.77	26.30	152	4319	541373	90082603
Skin exfoliation	113.94	26.30	59	4412	67854	90556122
Rash	98.59	26.30	155	4316	795945	89828031
Sleep disorder due to a general medical condition	84.12	26.30	42	4429	44696	90579280
Therapeutic response shortened	79.63	26.30	33	4438	22846	90601130
Psoriasis	69.87	26.30	58	4413	147696	90476280
Skin fissures	65.68	26.30	28	4443	20781	90603195
Erythema	63.86	26.30	67	4404	229179	90394797
Product use in unapproved indication	62.91	26.30	80	4391	336156	90287820
Injection site pain	61.76	26.30	58	4413	173641	90450335
Steroid withdrawal syndrome	58.68	26.30	12	4459	664	90623312
Drug ineffective for unapproved indication	51.18	26.30	35	4436	66609	90557367
Product dose omission issue	41.74	26.30	61	4410	291626	90332350
Treatment failure	41.25	26.30	62	4409	303866	90320110
Lymphadenitis	41.23	26.30	13	4458	4124	90619852
Dry eye	41.13	26.30	29	4442	57902	90566074
Wound complication	39.43	26.30	13	4458	4750	90619226
Subcutaneous abscess	38.87	26.30	14	4457	6652	90617324
Skin burning sensation	38.58	26.30	19	4452	19592	90604384
Impaired quality of life	38.45	26.30	20	4451	23124	90600852
Incorrect dose administered	37.29	26.30	31	4440	78899	90545077
Eye pruritus	36.87	26.30	21	4450	29006	90594970
Skin plaque	36.77	26.30	15	4456	9960	90614016
Rash pruritic	36.19	26.30	31	4440	82183	90541793
Application site pain	31.65	26.30	11	4460	4709	90619267
Skin haemorrhage	31.34	26.30	17	4454	21363	90602613
Eye irritation	31.30	26.30	20	4451	33958	90590018
Product availability issue	30.29	26.30	12	4459	7392	90616584
Therapeutic response decreased	30.00	26.30	29	4442	89700	90534276
Neurodermatitis	28.02	26.30	9	4462	3029	90620947
Conjunctivitis	27.82	26.30	17	4454	26689	90597287
Ocular hyperaemia	26.52	26.30	18	4453	33780	90590196

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
Dermatitis atopic	302.11	40.66	77	1900	12327	42607031
Drug ineffective	142.19	40.66	158	1819	630039	41989319
Pruritus	134.93	40.66	92	1885	188679	42430679
Treatment failure	98.63	40.66	51	1926	62573	42556785
Eczema	78.40	40.66	36	1941	34050	42585308
Skin exfoliation	65.78	40.66	34	1943	41519	42577839
Rash	64.10	40.66	71	1906	276883	42342475
Dry skin	60.94	40.66	34	1943	48304	42571054
Sleep disorder due to a general medical condition	54.91	40.66	23	1954	17430	42601928
Psoriasis	50.10	40.66	30	1947	48574	42570784
Discomfort	46.80	40.66	23	1954	25196	42594162
Papule	41.58	40.66	14	1963	5812	42613546

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
Dermatitis atopic	525.06	26.52	136	4528	25405	110559230
Pruritus	159.02	26.52	156	4508	581404	110003231
Eczema	156.05	26.52	71	4593	72222	110512413
Drug ineffective	140.22	26.52	237	4427	1520303	109064332
Dry skin	132.02	26.52	72	4592	107581	110477054
Rash	124.37	26.52	162	4502	820802	109763833
Skin exfoliation	92.09	26.52	53	4611	87598	110497037
Sleep disorder due to a general medical condition	90.24	26.52	44	4620	52068	110532567
Steroid withdrawal syndrome	86.02	26.52	17	4647	928	110583707
Treatment failure	84.11	26.52	79	4585	277155	110307480
Psoriasis	71.67	26.52	54	4610	139939	110444696
Therapeutic response shortened	66.74	26.52	30	4634	29553	110555082
Skin fissures	65.54	26.52	28	4636	24430	110560205
Eye pruritus	60.73	26.52	29	4635	32746	110551889
Erythema	59.23	26.52	67	4597	291380	110293255
Lichen nitidus	56.24	26.52	9	4655	143	110584492
Drug ineffective for unapproved indication	55.58	26.52	41	4623	102797	110481838
Ocular hyperaemia	52.90	26.52	28	4636	39258	110545377
Product dose omission issue	52.26	26.52	66	4598	321716	110262919
Androgenetic alopecia	51.11	26.52	9	4655	260	110584375
Injection site pain	50.63	26.52	49	4615	177873	110406762
Eye irritation	48.34	26.52	25	4639	33427	110551208
Application site pain	43.66	26.52	14	4650	5485	110579150
Rash pruritic	41.86	26.52	34	4630	98035	110486600
Limbic encephalitis	41.23	26.52	9	4655	799	110583836
Chronic cutaneous lupus erythematosus	39.15	26.52	9	4655	1010	110583625
Dry eye	36.49	26.52	25	4639	55768	110528867
Incorrect dose administered	34.18	26.52	31	4633	103610	110481025
Impaired quality of life	33.76	26.52	19	4645	29998	110554637
Intertrigo	32.31	26.52	8	4656	1230	110583405
Product use in unapproved indication	32.04	26.52	63	4601	447314	110137321
Pain of skin	31.93	26.52	16	4648	20013	110564622
Skin haemorrhage	31.46	26.52	17	4647	24810	110559825
Product availability issue	31.37	26.52	12	4652	7878	110576757
Skin burning sensation	30.63	26.52	16	4648	21809	110562826
Inappropriate schedule of product administration	30.23	26.52	40	4624	203597	110381038
Therapeutic response decreased	30.13	26.52	28	4636	96471	110488164
Discomfort	30.09	26.52	41	4623	214666	110369969
Rosacea	28.36	26.52	10	4654	5226	110579409
Dermatitis contact	27.84	26.52	13	4651	13940	110570695
Tinea versicolour	26.94	26.52	6	4658	584	110584051

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pimecrolimus 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Description:

Drug dosage:

ADMET properties:

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Approvals:

FDA Adverse Event Reporting System (Female)

FDA Adverse Event Reporting System (Male)

FDA Adverse Event Reporting System (Geriatric)

FDA Adverse Event Reporting System (Pediatric)

Pharmacologic Action:

Related Drugs by ATC class:

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

🐶 Veterinary Drug Use

🐶 Veterinary products

Acid dissociation constants calculated using MoKa v3.0.0

Orange Book patent data (new drug applications)

Orange Book exclusivity data (new drug applications)

Bioactivity Summary:

External reference:

Pharmaceutical products:

Source	Code	Description
ATC	D11AH02	DERMATOLOGICALS OTHER DERMATOLOGICAL PREPARATIONS OTHER DERMATOLOGICAL PREPARATIONS Agents for dermatitis, excluding corticosteroids
FDA EPC	N0000175457	Calcineurin Inhibitor Immunosuppressant
FDA MoA	N0000175458	Calcineurin Inhibitors
MeSH PA	D000700	Analgesics
MeSH PA	D000893	Anti-Inflammatory Agents
MeSH PA	D000894	Anti-Inflammatory Agents, Non-Steroidal
MeSH PA	D003879	Dermatologic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D007155	Immunologic Factors
MeSH PA	D007166	Immunosuppressive Agents
MeSH PA	D018373	Peripheral Nervous System Agents
MeSH PA	D018501	Antirheumatic Agents
MeSH PA	D018689	Sensory System Agents
MeSH PA	D018712	Analgesics, Non-Narcotic
MeSH PA	D065095	Calcineurin Inhibitors
CHEBI has role	CHEBI:50177	dermatologic drug
CHEBI has role	CHEBI:66981	ophthalmology drug

Disease	Relation	SNOMED_ID	DOID
Atopic dermatitis	indication	24079001	DOID:3310
Intractable Eczema	indication
Herpes zoster	contraindication	4740000	DOID:8536
Lymphadenopathy	contraindication	30746006
Immunosuppression	contraindication	38013005
Varicella	contraindication	38907003	DOID:8659
Verruca vulgaris	contraindication	57019003	DOID:11165
Herpes simplex	contraindication	88594005	DOID:8566
Viral infection of skin	contraindication	128937004
Eczema herpeticum	contraindication	186535001	DOID:9123
Infectious mononucleosis	contraindication	271558008	DOID:8568
Netherton's syndrome	contraindication	312514006
Impetiginized atopic dermatitis	contraindication	402201001
Pre-Malignant Skin Lesion	contraindication

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Peptidyl-prolyl cis-trans isomerase FKBP1A	Enzyme	P62942	FKB1A_HUMAN	INHIBITOR	Kd	9	WOMBAT-PK	CHEMBL
Interleukin-2	Cytokine	P60568	IL2_HUMAN				WOMBAT-PK
Interleukin-5	Cytokine	P05113	IL5_HUMAN				WOMBAT-PK
Interferon gamma	Cytokine	P01579	IFNG_HUMAN				WOMBAT-PK
Serine/threonine-protein phosphatase 2B catalytic subunit gamma isoform	Enzyme	P48454	PP2BC_HUMAN				WOMBAT-PK
Peptidyl-prolyl cis-trans isomerase FKBP1A	Enzyme		FKB1A_RAT	INHIBITOR	IC50	8.22	IUPHAR

ID	Source
4021291	VUID
N0000148728	NUI
D05480	KEGG_DRUG
4021291	VANDF
C1099414	UMLSCUI
CHEBI:135888	CHEBI
CHEMBL1200686	ChEMBL_ID
DB00337	DRUGBANK_ID
C117268	MESH_SUPPLEMENTAL_RECORD_UI
6783	IUPHAR_LIGAND_ID
7632	INN_ID
7KYV510875	UNII
6509979	PUBCHEM_CID
306865	RXNORM
16235	MMSL
302773	MMSL
42597	MMSL
009525	NDDF
385580005	SNOMEDCT_US
385581009	SNOMEDCT_US
7KYV510875	INXIGHT DRUGS

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
pimecrolimus	HUMAN PRESCRIPTION DRUG LABEL	1	0591-2944	CREAM	10 mg	TOPICAL	ANDA	25 sections
Elidel	HUMAN PRESCRIPTION DRUG LABEL	1	54868-4878	CREAM	10 mg	TOPICAL	NDA	25 sections
Pimecrolimus	HUMAN PRESCRIPTION DRUG LABEL	1	68462-609	CREAM	10 mg	TOPICAL	ANDA	25 sections
Pimecrolimus	HUMAN PRESCRIPTION DRUG LABEL	1	68462-609	CREAM	10 mg	TOPICAL	ANDA	25 sections
Pimecrolimus	HUMAN PRESCRIPTION DRUG LABEL	1	68682-110	CREAM	10 mg	TOPICAL	NDA authorized generic	27 sections
Pimecrolimus	HUMAN PRESCRIPTION DRUG LABEL	1	68682-111	CREAM	10 mg	TOPICAL	NDA authorized generic	27 sections
Pimecrolimus	HUMAN PRESCRIPTION DRUG LABEL	1	68682-112	CREAM	10 mg	TOPICAL	NDA authorized generic	27 sections
Pimecrolimus	HUMAN PRESCRIPTION DRUG LABEL	1	71335-2988	CREAM	10 mg	TOPICAL	NDA authorized generic	26 sections

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	12.4	acidic
pKa2	13.57	acidic