All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

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

Molfile Inchi Smiles Synonyms: lotilaner credelio

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). Molecular weight: 596.75 Formula: C20H14Cl3F6N3O3S CLOGP: 5.13 LIPINSKI: 2 HAC: 6 HDO: 2 TPSA: 79.79 ALOGS: -6.13 ROTB: 8 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
kinase-safety-class	ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,GSK3B,ITK,JAK2,MAP2K6,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MET,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM2,PRKDC,STK33,SYK,TEK,TTK,ZAP70	40
kinase-selectivity-class	GRK2,PDK1,PDK4	3
pfas-class	PFAS structural alert (1 = True, 0 = False)	1

Approvals:

Date	Agency	Company	Orphan
July 24, 2023	FDA	TARSUS

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
Eye irritation	521.27	85.68	113	1048	33865	90593421
Instillation site irritation	266.81	85.68	32	1129	191	90627095
Ocular hyperaemia	232.90	85.68	59	1102	33739	90593547
Vision blurred	187.06	85.68	65	1096	110228	90517058
Eye pain	175.71	85.68	50	1111	44118	90583168
Eye pruritus	172.06	85.68	45	1116	28982	90598304
Lacrimation increased	118.15	85.68	33	1128	27029	90600257
Eye swelling	97.72	85.68	29	1132	29357	90597929
Eye discharge	95.74	85.68	22	1139	8236	90619050

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
Instillation site irritation	185.29	94.96	19	300	37	42620979
Eye irritation	153.61	94.96	31	288	11287	42609729

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
Eye irritation	600.91	98.34	124	1127	33328	110554720
Instillation site irritation	377.62	98.34	42	1209	131	110587917
Ocular hyperaemia	271.30	98.34	67	1184	39219	110548829
Vision blurred	220.13	98.34	74	1177	128948	110459100
Eye pain	203.04	98.34	56	1195	50043	110538005
Eye pruritus	201.54	98.34	51	1200	32724	110555324
Lacrimation increased	136.33	98.34	37	1214	30913	110557135
Eye discharge	119.20	98.34	26	1225	8728	110579320
Eye swelling	102.28	98.34	30	1221	33018	110555030

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	S01AX25	SENSORY ORGANS OPHTHALMOLOGICALS ANTIINFECTIVES Other antiinfectives
MeSH PA	D000890	Anti-Infective Agents
MeSH PA	D000977	Antiparasitic Agents
FDA EPC	N0000194050	Ectoparasiticide
CHEBI has role	CHEBI:38956	ectoparasiticide
CHEBI has role	CHEBI:38999	GABA-gated chloride channel antagonist
CHEBI has role	CHEBI:66981	ophthalmology drug

Related Drugs by ATC class:

S01AX Other antiinfectives 13 drugs

bibrocatholcethexoniumchlorhexidinedibrompropamidinehexamidinenitrofurazonepicloxydinepolihexanidepovidone-iodinepropamidineresorcinolsodium borate show all 13 →

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)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
0.25%	XDEMVY	TARSUS	N217603	July 24, 2023	RX	SOLUTION/DROPS	OPHTHALMIC	10835517	Dec. 14, 2038	TREATMENT OF DEMODEX BLEPHARITIS VIA TOPICAL ADMINISTRATION TO AN OCULAR SURFACE
0.25%	XDEMVY	TARSUS	N217603	July 24, 2023	RX	SOLUTION/DROPS	OPHTHALMIC	11197847	Dec. 14, 2038	TREATMENT OF DEMODEX BLEPHARITIS VIA TOPICAL ADMINISTRATION TO AN OCULAR SURFACE
0.25%	XDEMVY	TARSUS	N217603	July 24, 2023	RX	SOLUTION/DROPS	OPHTHALMIC	11690826	Dec. 14, 2038	TREATMENT OF DEMODEX BLEPHARITIS VIA TOPICAL ADMINISTRATION TO AN OCULAR SURFACE
0.25%	XDEMVY	TARSUS	N217603	July 24, 2023	RX	SOLUTION/DROPS	OPHTHALMIC	11690827	Dec. 14, 2038	TREATMENT OF DEMODEX BLEPHARITIS VIA TOPICAL ADMINISTRATION TO AN OCULAR SURFACE
0.25%	XDEMVY	TARSUS	N217603	July 24, 2023	RX	SOLUTION/DROPS	OPHTHALMIC	12171750	Dec. 14, 2038	TREATMENT OF DEMODEX BLEPHARITIS VIA TOPICAL ADMINISTRATION TO AN OCULAR SURFACE

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
0.25%	XDEMVY	TARSUS	N217603	July 24, 2023	RX	SOLUTION/DROPS	OPHTHALMIC	July 24, 2028	NEW CHEMICAL ENTITY

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
GABA-A receptor	Ion channel		E0V9W2_PEDHC E0VY07_PEDHC E0W492_PEDHC	INHIBITOR				UNKNOWN	DRUG LABEL

External reference:

ID	Source
CHEBI:229657	CHEBI
CHEMBL3707310	ChEMBL_ID
C000711088	MESH_SUPPLEMENTAL_RECORD_UI
4042449	VANDF
C4550692	UMLSCUI
9867	INN_ID
D11212	KEGG_DRUG
76959255	PUBCHEM_CID
41836	MMSL
017865	NDDF
HEH4938D7K	UNII
1998841	RXNORM

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