Stem definition | Drug id | CAS RN |
---|---|---|
immunosuppressants, rapamycin derivatives | 2168 | 137071-32-0 |
None
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 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
BA (Bioavailability) | 0 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Date | Agency | Company | Orphan |
---|---|---|---|
Dec. 13, 2001 | FDA | VALEANT BERMUDA |
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 |
---|---|---|---|---|---|---|
Application site pain | 85.82 | 23.94 | 22 | 2186 | 3776 | 50599140 |
Steroid withdrawal syndrome | 63.15 | 23.94 | 12 | 2196 | 515 | 50602401 |
Application site erythema | 54.53 | 23.94 | 16 | 2192 | 4522 | 50598394 |
Psoriasis | 54.11 | 23.94 | 35 | 2173 | 68965 | 50533951 |
Eczema | 50.44 | 23.94 | 23 | 2185 | 22679 | 50580237 |
Dermatitis atopic | 40.27 | 23.94 | 12 | 2196 | 3574 | 50599342 |
Application site pruritus | 39.71 | 23.94 | 12 | 2196 | 3747 | 50599169 |
Application site irritation | 39.65 | 23.94 | 10 | 2198 | 1605 | 50601311 |
Skin burning sensation | 31.37 | 23.94 | 13 | 2195 | 10172 | 50592744 |
Vulval disorder | 30.99 | 23.94 | 7 | 2201 | 703 | 50602213 |
Skin exfoliation | 28.66 | 23.94 | 18 | 2190 | 33594 | 50569322 |
Application site swelling | 27.76 | 23.94 | 6 | 2202 | 492 | 50602424 |
Application site dryness | 27.58 | 23.94 | 5 | 2203 | 165 | 50602751 |
Pruritus | 27.04 | 23.94 | 46 | 2162 | 283522 | 50319394 |
Lymphadenopathy | 26.23 | 23.94 | 17 | 2191 | 33482 | 50569434 |
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 |
---|---|---|---|---|---|---|
Application site pain | 41.88 | 30.75 | 10 | 984 | 1669 | 29571864 |
Dermatitis atopic | 39.11 | 30.75 | 10 | 984 | 2209 | 29571324 |
Limbic encephalitis | 37.33 | 30.75 | 7 | 987 | 365 | 29573168 |
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 |
---|---|---|---|---|---|---|
Application site pain | 107.76 | 24.18 | 26 | 2302 | 4222 | 64492182 |
Steroid withdrawal syndrome | 95.04 | 24.18 | 17 | 2311 | 633 | 64495771 |
Application site erythema | 70.94 | 24.18 | 19 | 2309 | 4670 | 64491734 |
Limbic encephalitis | 44.30 | 24.18 | 9 | 2319 | 662 | 64495742 |
Eczema | 42.62 | 24.18 | 21 | 2307 | 29699 | 64466705 |
Dermatitis atopic | 41.59 | 24.18 | 12 | 2316 | 3864 | 64492540 |
Application site pruritus | 38.17 | 24.18 | 11 | 2317 | 3528 | 64492876 |
Skin burning sensation | 36.84 | 24.18 | 14 | 2314 | 10569 | 64485835 |
Application site irritation | 36.65 | 24.18 | 9 | 2319 | 1567 | 64494837 |
Pruritus | 33.10 | 24.18 | 48 | 2280 | 312352 | 64184052 |
Application site vesicles | 33.04 | 24.18 | 8 | 2320 | 1314 | 64495090 |
Application site swelling | 33.01 | 24.18 | 7 | 2321 | 635 | 64495769 |
Psoriasis | 32.14 | 24.18 | 24 | 2304 | 71679 | 64424725 |
Ocular hyperaemia | 29.56 | 24.18 | 15 | 2313 | 22549 | 64473855 |
Erythema | 29.52 | 24.18 | 35 | 2293 | 187035 | 64309369 |
Application site dryness | 28.13 | 24.18 | 5 | 2323 | 179 | 64496225 |
Application site dermatitis | 28.10 | 24.18 | 5 | 2323 | 180 | 64496224 |
Skin exfoliation | 27.02 | 24.18 | 18 | 2310 | 44867 | 64451537 |
Eye swelling | 26.84 | 24.18 | 14 | 2314 | 22267 | 64474137 |
Application site discolouration | 26.69 | 24.18 | 6 | 2322 | 714 | 64495690 |
Lymphadenopathy | 26.38 | 24.18 | 18 | 2310 | 46668 | 64449736 |
Eye pruritus | 24.47 | 24.18 | 11 | 2317 | 12648 | 64483756 |
None
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 | D018712 | Analgesics, Non-Narcotic |
MeSH PA | D000893 | Anti-Inflammatory Agents |
MeSH PA | D000894 | Anti-Inflammatory Agents, Non-Steroidal |
MeSH PA | D018501 | Antirheumatic Agents |
MeSH PA | D065095 | Calcineurin Inhibitors |
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 | D018689 | Sensory System Agents |
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 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 12.4 | acidic |
pKa2 | 13.57 | acidic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Peptidyl-prolyl cis-trans isomerase FKBP1A | Enzyme | INHIBITOR | Kd | 9 | WOMBAT-PK | CHEMBL | |||
Interleukin-5 | Cytokine | WOMBAT-PK | |||||||
Interferon gamma | Cytokine | WOMBAT-PK | |||||||
Interleukin-2 | Cytokine | WOMBAT-PK | |||||||
Serine/threonine-protein phosphatase 2B catalytic subunit gamma isoform | Enzyme | WOMBAT-PK | |||||||
Peptidyl-prolyl cis-trans isomerase FKBP1A | Enzyme | 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 |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
ELIDEL | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0187-5100 | CREAM | 10 mg | TOPICAL | NDA | 27 sections |
ELIDEL | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0187-5101 | CREAM | 10 mg | TOPICAL | NDA | 27 sections |
ELIDEL | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0187-5102 | CREAM | 10 mg | TOPICAL | NDA | 27 sections |
ELIDEL | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0187-5103 | CREAM | 10 mg | TOPICAL | NDA | 27 sections |
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 | 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 | 70518-2292 | CREAM | 10 mg | TOPICAL | ANDA | 25 sections |