pimecrolimus 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 | 86.77 | 23.18 | 22 | 1821 | 4001 | 46680218 |
| Psoriasis | 58.12 | 23.18 | 37 | 1806 | 78567 | 46605652 |
| Application site erythema | 54.90 | 23.18 | 16 | 1827 | 4888 | 46679331 |
| Steroid withdrawal syndrome | 52.51 | 23.18 | 10 | 1833 | 481 | 46683738 |
| Eczema | 41.95 | 23.18 | 19 | 1824 | 20381 | 46663838 |
| Application site pruritus | 40.13 | 23.18 | 12 | 1831 | 4001 | 46680218 |
| Application site irritation | 39.46 | 23.18 | 10 | 1833 | 1809 | 46682410 |
| Application site dryness | 28.11 | 23.18 | 5 | 1838 | 164 | 46684055 |
| Lymphadenopathy | 27.81 | 23.18 | 17 | 1826 | 33471 | 46650748 |
| Application site swelling | 27.53 | 23.18 | 6 | 1837 | 566 | 46683653 |
| Skin burning sensation | 25.32 | 23.18 | 11 | 1832 | 10681 | 46673538 |
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 | 43.26 | 28.90 | 10 | 875 | 1653 | 29949940 |
| Dermatitis atopic | 36.38 | 28.90 | 8 | 877 | 1056 | 29950537 |
| Application site erythema | 30.24 | 28.90 | 8 | 877 | 2295 | 29949298 |
| Insulin resistance | 29.38 | 28.90 | 6 | 879 | 556 | 29951037 |
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 (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 |
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 | |||
| Serine/threonine-protein phosphatase 2B catalytic subunit gamma isoform | Enzyme | WOMBAT-PK | |||||||
| Interleukin-2 | Cytokine | WOMBAT-PK | |||||||
| Interferon gamma | Cytokine | WOMBAT-PK | |||||||
| Interleukin-5 | Cytokine | WOMBAT-PK | |||||||
| Peptidyl-prolyl cis-trans isomerase FKBP1A | Unclassified | INHIBITOR | IC50 | 8.22 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| 4021291 | VUID |
| N0000148728 | NUI |
| D05480 | KEGG_DRUG |
| 4021291 | VANDF |
| C0971833 | UMLSCUI |
| CHEBI:135888 | CHEBI |
| CHEMBL1200686 | ChEMBL_ID |
| DB00337 | DRUGBANK_ID |
| C117268 | MESH_SUPPLEMENTAL_RECORD_UI |
| 6509979 | PUBCHEM_CID |
| 6783 | IUPHAR_LIGAND_ID |
| 7632 | INN_ID |
| 7KYV510875 | UNII |
| 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 |