pimecrolimus 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| immunosuppressants, rapamycin derivatives | 2168 | 137071-32-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
an ascomycin derivative; mechanism of action involves calcineurin inhibition, blockage of T cell activation, blocking signal transduction pathways in T cells, and inhibition of the synthesis of inflammatory cytokines, specifically Th1- and Th2-type cytokines
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| 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 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 13, 2001 | FDA | VALEANT BERMUDA |
FDA Adverse Event Reporting System (Female)
| 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 |
FDA Adverse Event Reporting System (Male)
| 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 |
FDA Adverse Event Reporting System (Geriatric)
| 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 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| 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 |
Drug Use | Suggest Off label Use Form| |View source of the data|
| 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 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 12.4 | acidic |
| pKa2 | 13.57 | acidic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| 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 |
External reference:
| 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 |
Pharmaceutical products:
| 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 |