lotilaner 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antagonists of GABA (gamma-aminobutyric acid) regulated chloride channels, antiparasitic agents | 5567 | 1369852-71-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Lotilaner is a gamma-aminobutyric acid (GABA)-gated chloride channel inhibitor selective for mites. Inhibition of these GABA chloride channels causes a paralytic action in the target organism leading to its death. Lotilaner is not an inhibitor of mammalian GABA mediated chloride channels when tested at up to 30 microM (18 microg/mL) in vitro (approximately 1100 times the RHOD).
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 24, 2023 | FDA | TARSUS |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
None
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Demodex blepharitis | indication | 403152000 |
🐶 Veterinary Drug Use
| Species | Use | Relation |
|---|---|---|
| Dogs | Flea infestations caused by Ctenocephalides felis | Indication |
| Dogs | Treatment and control of tick infestations with Amblyomma americanum (lone star tick) | Indication |
| Dogs | Treatment and control of tick infestations with Dermacentor variabilis (American dog tick) | Indication |
| Dogs | Treatment and control of tick infestations with Ixodes scapularis (black-legged tick) | Indication |
| Dogs | Treatment and control of tick infestations with Rhipicephalus sanguineus (brown dog tick) | Indication |
🐶 Veterinary products
| Product | Applicant | Ingredients |
|---|---|---|
| Credelio | Elanco US Inc. | 1 |
| Credelio CAT | Elanco US Inc. | 1 |
Acid dissociation constants calculated using MoKa v3.0.0
None
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 |
|---|---|---|---|---|---|---|---|---|---|
| GABA-A receptor | Ion channel | INHIBITOR | UNKNOWN | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| CHEMBL3707310 | ChEMBL_ID |
| C000711088 | MESH_SUPPLEMENTAL_RECORD_UI |
| 017865 | NDDF |
| C4550692 | UMLSCUI |
| 9867 | INN_ID |
| D11212 | KEGG_DRUG |
| 76959255 | PUBCHEM_CID |
| 1998841 | RXNORM |
| 41836 | MMSL |
| HEH4938D7K | UNII |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| XDEMVY | HUMAN PRESCRIPTION DRUG LABEL | 1 | 81942-125 | SOLUTION/ DROPS | 2.50 mg | OPHTHALMIC | NDA | 24 sections |