Tirbanibulin

Details

Stereochemistry	ACHIRAL
Molecular Formula	C26H29N3O3
Molecular Weight	431.5268
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

O=C(CC1=NC=C(C=C1)C2=CC=C(OCCN3CCOCC3)C=C2)NCC4=CC=CC=C4

InChI

InChIKey=HUNGUWOZPQBXGX-UHFFFAOYSA-N

InChI=1S/C26H29N3O3/c30-26(28-19-21-4-2-1-3-5-21)18-24-9-6-23(20-27-24)22-7-10-25(11-8-22)32-17-14-29-12-15-31-16-13-29/h1-11,20H,12-19H2,(H,28,30)

HIDE SMILES / InChI

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23314737 | https://www.ncbi.nlm.nih.gov/pubmed/27737538

KX-01 is a dual inhibitor of Src kinase and tubulin polymerization. KX01 promotes the induction of p53, G2/M arrest of proliferating cell populations and subsequent apoptosis via the stimulation of Caspase-3 and PARP cleavage. The drug was developed by Kinex Pharmaceuticals and reached phase II of clinical trials for the treatment of Castration-Resistant Prostate Cancer and Actinic Keratosis. KX-01 demonstrated good in vitro pofile against different cancer cell lines with IC50 in nanomolar range.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Tyrosine-protein kinase SRC 19 Target ID: CHEMBL267 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23314737 \| https://www.ncbi.nlm.nih.gov/pubmed/27737538	Inhibitor 8504
tubulin complex assembly 1 Target ID: GO:0007021 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23314737 \| https://www.ncbi.nlm.nih.gov/pubmed/27737538	Inhibitor 8504

Conditions

Condition	Modality	Targets	Highest Phase	Product
Castrate-resistant prostate cancer 20 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23314737	Primary		Phase II 1147	Unknown Approved Use Unknown
Actinic keratosis 12 Sources: https://clinicaltrials.gov/ct2/show/NCT02838628	Primary		Phase II 1147	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
0.34 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/34783452/	250 mg 1 times / day multiple, topical dose: 250 mg route of administration: Topical experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.18 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/34783452/	250 mg 1 times / day multiple, topical dose: 250 mg route of administration: Topical experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
0.26 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/34783452/	250 mg 1 times / day multiple, topical dose: 250 mg route of administration: Topical experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3.61 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	2 mg 2 times / day multiple, oral dose: 2 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3.73 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	2 mg 2 times / day multiple, oral dose: 2 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
9.55 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	5 mg 2 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
16.6 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	5 mg 2 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
26.45 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	10 mg 2 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
14.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	10 mg 2 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
37.85 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	20 mg 2 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
33.85 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	20 mg 2 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
79.75 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	40 mg 2 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
73.1 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	40 mg 2 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
58.7 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	40 mg 2 times / day steady-state, oral dose: 40 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
60.5 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	40 mg 2 times / day steady-state, oral dose: 40 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
188 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	50 mg 2 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
21.7 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	50 mg 2 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
117 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	60 mg 2 times / day steady-state, oral dose: 60 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
98.6 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	60 mg 2 times / day steady-state, oral dose: 60 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
273 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	80 mg 2 times / day steady-state, oral dose: 80 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
143.3 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	80 mg 2 times / day steady-state, oral dose: 80 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
5 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/34783452/	250 mg 1 times / day multiple, topical dose: 250 mg route of administration: Topical experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3.18 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/34783452/	250 mg 1 times / day multiple, topical dose: 250 mg route of administration: Topical experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
4.09 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/34783452/	250 mg 1 times / day multiple, topical dose: 250 mg route of administration: Topical experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
15.39 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	2 mg 2 times / day multiple, oral dose: 2 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
16.28 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	2 mg 2 times / day multiple, oral dose: 2 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
31 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	5 mg 2 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
85.95 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	5 mg 2 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
68.65 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	10 mg 2 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
58.48 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	10 mg 2 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
143.79 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	20 mg 2 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
104.49 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	20 mg 2 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
332.97 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	40 mg 2 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
336.09 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	40 mg 2 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
196.78 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	40 mg 2 times / day steady-state, oral dose: 40 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
166.75 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	40 mg 2 times / day steady-state, oral dose: 40 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1898.74 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	50 mg 2 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
94.2 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	50 mg 2 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
360.42 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	60 mg 2 times / day steady-state, oral dose: 60 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
298.27 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	60 mg 2 times / day steady-state, oral dose: 60 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
984.8 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	80 mg 2 times / day steady-state, oral dose: 80 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
560.25 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	80 mg 2 times / day steady-state, oral dose: 80 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
1 day EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/34783452/	250 mg 1 times / day multiple, topical dose: 250 mg route of administration: Topical experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3.95 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	2 mg 2 times / day multiple, oral dose: 2 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3.45 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	2 mg 2 times / day multiple, oral dose: 2 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3.01 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	5 mg 2 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4.95 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	5 mg 2 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2.98 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	10 mg 2 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2.96 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	10 mg 2 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
5.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	20 mg 2 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3.52 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	20 mg 2 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3.47 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	40 mg 2 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4.53 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	40 mg 2 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	40 mg 2 times / day steady-state, oral dose: 40 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4.63 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	40 mg 2 times / day steady-state, oral dose: 40 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
9.34 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	50 mg 2 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3.22 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	50 mg 2 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
3.77 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	60 mg 2 times / day steady-state, oral dose: 60 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4.67 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	60 mg 2 times / day steady-state, oral dose: 60 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2.89 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	80 mg 2 times / day steady-state, oral dose: 80 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
5.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23361621/	80 mg 2 times / day steady-state, oral dose: 80 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	KX-01 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
17% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23314737/			KX-01 serum	Homo sapiens

Doses

Dose	Population	Adverse events
80 mg 2 times / day multiple, oral Highest studied dose Dose: 80 mg, 2 times / day Route: oral Route: multiple Dose: 80 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/	DLT: Neutropenia, AST increased... Dose limiting toxicities: Neutropenia (grade 4, 33.3%) AST increased (grade 3, 33.3%) Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/
40 mg 2 times / day multiple, oral MTD Dose: 40 mg, 2 times / day Route: oral Route: multiple Dose: 40 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/	Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/
1 % 1 times / day multiple, topical Recommended Dose: 1 %, 1 times / day Route: topical Route: multiple Dose: 1 %, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/33567191/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/33567191/	Sources: https://pubmed.ncbi.nlm.nih.gov/33567191/
50 mg 2 times / day multiple, oral Studied dose Dose: 50 mg, 2 times / day Route: oral Route: multiple Dose: 50 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/	DLT: AST increased, Thrombocytopenia... Dose limiting toxicities: AST increased (grade 3, 25%) Thrombocytopenia (grade 3, 25%) Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/
60 mg 2 times / day multiple, oral Studied dose Dose: 60 mg, 2 times / day Route: oral Route: multiple Dose: 60 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/	DLT: AST increased, ALT increased... Dose limiting toxicities: AST increased (grade 3, 16.7%) ALT increased (grade 3, 16.7%) Neutropenia (grade 4, 16.7%) Fatigue (grade 3, 16.7%) Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/

AEs

AE	Significance	Dose	Population
AST increased	grade 3, 33.3% DLT, Disc. AE	80 mg 2 times / day multiple, oral Highest studied dose Dose: 80 mg, 2 times / day Route: oral Route: multiple Dose: 80 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/
Neutropenia	grade 4, 33.3% DLT, Disc. AE	80 mg 2 times / day multiple, oral Highest studied dose Dose: 80 mg, 2 times / day Route: oral Route: multiple Dose: 80 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/
AST increased	grade 3, 25% DLT, Disc. AE	50 mg 2 times / day multiple, oral Studied dose Dose: 50 mg, 2 times / day Route: oral Route: multiple Dose: 50 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/
Thrombocytopenia	grade 3, 25% DLT, Disc. AE	50 mg 2 times / day multiple, oral Studied dose Dose: 50 mg, 2 times / day Route: oral Route: multiple Dose: 50 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/
ALT increased	grade 3, 16.7% DLT, Disc. AE	60 mg 2 times / day multiple, oral Studied dose Dose: 60 mg, 2 times / day Route: oral Route: multiple Dose: 60 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/
AST increased	grade 3, 16.7% DLT, Disc. AE	60 mg 2 times / day multiple, oral Studied dose Dose: 60 mg, 2 times / day Route: oral Route: multiple Dose: 60 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/
Fatigue	grade 3, 16.7% DLT, Disc. AE	60 mg 2 times / day multiple, oral Studied dose Dose: 60 mg, 2 times / day Route: oral Route: multiple Dose: 60 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/
Neutropenia	grade 4, 16.7% DLT, Disc. AE	60 mg 2 times / day multiple, oral Studied dose Dose: 60 mg, 2 times / day Route: oral Route: multiple Dose: 60 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/23361621/

PubMed

Title	Date	PubMed
A phase I trial of KX2-391, a novel non-ATP competitive substrate-pocket- directed SRC inhibitor, in patients with advanced malignancies.	2013-08	23361621
KX-01, a novel Src kinase inhibitor directed toward the peptide substrate site, synergizes with tamoxifen in estrogen receptor α positive breast cancer.	2012-04	21509526
Thiazolyl N-benzyl-substituted acetamide derivatives: synthesis, Src kinase inhibitory and anticancer activities.	2011-10	21852023
Synthesis and pharmacological evaluation of thieno[2,3-b]pyridine derivatives as novel c-Src inhibitors.	2011-04-15	21459579
Expression of Src and FAK in hepatocellular carcinoma and the effect of Src inhibitors on hepatocellular carcinoma in vitro.	2009-07	18979199

Patents

Sample Use Guides

In Vivo Use Guide

Patients recieve 40 mg of oral KX-01 twice-daily. Ointment form should be applied once daily.

Route of Administration: Other

In Vitro Use Guide

PC3-LN4 human prostate cancer cells were treated with 10(-4)-10(4) nM of KX-01 for 72 hours and GI50 value was determined to be 40 nM.

Name

Type

Language

Tirbanibulin

Official Name

English

KX-01

Preferred Name

English

KX2391

Code

English

KX-2-391

Code

English

KLISYRI

Brand Name

English

TIRBANIBULIN [ORANGE BOOK]

Common Name

English

Tirbanibulin [WHO-DD]

Common Name

English

2-PYRIDINEACETAMIDE, 5-(4-(2-(4-MORPHOLINYL)ETHOXY)PHENYL)-N-(PHENYLMETHYL)-

Systematic Name

English

N-BENZYL-2-(5-(4-(2-MORPHOLIN-4-YLETHOXY)PHENYL)PYRIDIN-2-YL)ACETAMIDE

Systematic Name

English

KX01

Code

English

tirbanibulin [INN]

Common Name

English

TIRBANIBULIN [USAN]

Common Name

English

KX-2391

Code

English

KX2-391

Code

English

Code System Code Type Description

FDA UNII

4V9848RS5G