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

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

Stem definition	Drug id	CAS RN
antineoplastics; mitotic inhibitors, tubulin binders	5431	897016-82-9

Description:

Molecule

Description

Molfile Inchi Smiles Synonyms: tirbanibulin tirbanibulin mesylate KX01 KX-01 KX2-391 klisyri ALM-14789

Tirbanibulin is a microtubule inhibitor developed for the topical treatment of actinic keratosis. The mechanism of action is not fully understood. However, it is known that tirbanibulin inhibits proliferation of keratinocytes through inhibition of tubulin polymerization and disruption of Src tyrosine kinase signaling. This results in disruption of the intracellular microtubule network, resulting in cell cycle arrest and apoptosis of keratinocytes. Molecular weight: 431.54 Formula: C26H29N3O3 CLOGP: 3.05 LIPINSKI: 0 HAC: 6 HDO: 1 TPSA: 63.69 ALOGS: -4.24 ROTB: 9 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
azlogd74	LogD at pH 7.4	2.854		High	1
caco2-efflux	Caco-2 efflux ratio (BA/AB)	0.755		High	1
caco2-intrinsic-papp	Caco-2 intrinsic apparent permeability	47.424	10^-6 cm/s	High	1
dh-clint	Dog hepatocyte intrinsic clearance	17.783	uL/min/10^6 cells	High	1
dppb	Dog plasma protein binding (% unbound)	13.550	%	High	1
fcs-ppb	Fetal calf serum protein binding (% unbound)	29.520	%	High	1
herg	hERG pIC50	4.884	pIC50	High	1
hh-clint	Human hepatocyte intrinsic clearance	7.962	uL/min/10^6 cells	High	1
hlm-clint	Human liver microsomal intrinsic clearance	91.622	uL/min/mg protein	High	1
hppb	Human plasma protein binding (% unbound)	7.860	%	High	1
kinase-safety-class	ACVR2B,AXL,BRAF,CAMK2D,CDK5,EIF2AK3,ERBB2,GRK2,ITK,PDK2,PDK4,PRKDC	12
mdck-mdr1-efflux	MDCK-MDR1 efflux ratio	2.296		High	1
mh-clint	Mouse hepatocyte intrinsic clearance	46.774		High	1
mppb	Mouse plasma protein binding (% unbound)	7.270		High	1
nih-mdck-mdr1-efflux	NIH MDCK-MDR1 efflux ratio	9.419		High	1
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
pppb	Pig plasma protein binding (% unbound)	15.670	%	High	1
rh-clint	Rat hepatocyte intrinsic clearance	62.951	uL/min/10^6 cells	High	1
rh-fuinc	Rat hepatocyte fraction unbound in incubation	65.740	%	High	1
rppb	Rat plasma protein binding (% unbound)	9.110	%	High	1
solubility-dd	Solubility at pH 7.4 in DMSO	92.683	uM	High	1

Approvals:

Date	Agency	Company	Orphan
Dec. 14, 2020	FDA	ALMIRALL
July 16, 2021	EMA	ALMIRALL S.A.

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:

Source	Code	Description
ATC	D06BX03	DERMATOLOGICALS ANTIBIOTICS AND CHEMOTHERAPEUTICS FOR DERMATOLOGICAL USE CHEMOTHERAPEUTICS FOR TOPICAL USE Other chemotherapeutics
MeSH PA	D004791	Enzyme Inhibitors
FDA PE	N0000175085	Microtubule Inhibition
FDA EPC	N0000175592	Microtubule Inhibitor
CHEBI has role	CHEBI:35610	antineoplastic agent
CHEBI has role	CHEBI:61951	microtubule-destabilising agent
CHEBI has role	CHEBI:68495	apoptosis inducer
CHEBI has role	CHEBI:76617	EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor

Related Drugs by ATC class:

D06BX Other chemotherapeutics 2 drugs

ingenol mebutatemetronidazole

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Actinic keratosis	indication	201101007	DOID:8866

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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
1%	KLISYRI	ALMIRALL	N213189	Dec. 14, 2020	RX	OINTMENT	TOPICAL	7851470	Feb. 2, 2029	TOPICAL TREATMENT OF ACTINIC KERATOSIS OF THE FACE OR SCALP
1%	KLISYRI	ALMIRALL	N213189	Dec. 14, 2020	RX	OINTMENT	TOPICAL	10617693	March 12, 2038	TOPICAL TREATMENT OF ACTINIC KERATOSIS OF THE FACE OR SCALP
1%	KLISYRI	ALMIRALL	N213189	Dec. 14, 2020	RX	OINTMENT	TOPICAL	11497750	March 12, 2038	TOPICAL TREATMENT OF ACTINIC KERATOSIS OF THE FACE OR SCALP

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
1%	KLISYRI	ALMIRALL	N213189	Dec. 14, 2020	RX	OINTMENT	TOPICAL	June 7, 2027	EXPANSION OF THE TREATMENT FIELD ON THE FACE OR SCALP UP TO 100 CM^2

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Tubulin beta chain	Structural	P07437	TBB5_HUMAN	INHIBITOR	Kd	5.90		SCIENTIFIC LITERATURE	DRUG LABEL
Proto-oncogene tyrosine-protein kinase Src	Kinase	P12931	SRC_HUMAN	INHIBITOR	IC50	4.34		IUPHAR
Tyrosine-protein kinase Lyn	Kinase	P07948	LYN_HUMAN		IC50	7		CHEMBL

External reference:

ID	Source
D11691	KEGG_DRUG
4V9848RS5G	UNII
1080645-95-9	SECONDARY_CAS_RN
C5239395	UMLSCUI
CHEBI:231702	CHEBI
DN0	PDB_CHEM_ID
CHEMBL571546	ChEMBL_ID
23635314	PUBCHEM_CID
DB06137	DRUGBANK_ID
CHEMBL4594279	ChEMBL_ID
10864	INN_ID
C000713668	MESH_SUPPLEMENTAL_RECORD_UI
7957	IUPHAR_LIGAND_ID
1144610005	SNOMEDCT_US
1144613007	SNOMEDCT_US
4039987	VANDF
342122	MMSL
39105	MMSL
018593	NDDF
2471078	RXNORM
4V9848RS5G	INXIGHT DRUGS

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Klisyri	HUMAN PRESCRIPTION DRUG LABEL	1	16110-391	OINTMENT	10 mg	TOPICAL	NDA	26 sections