CENOBAMATE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C10H10ClN5O2
Molecular Weight	267.672
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

NC(=O)O[C@@H](CN1N=CN=N1)C2=C(Cl)C=CC=C2

InChI

InChIKey=GFHAXPJGXSQLPT-VIFPVBQESA-N

InChI=1S/C10H10ClN5O2/c11-8-4-2-1-3-7(8)9(18-10(12)17)5-16-14-6-13-15-16/h1-4,6,9H,5H2,(H2,12,17)/t9-/m0/s1

HIDE SMILES / InChI

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/28799516 | https://www.ncbi.nlm.nih.gov/pubmed/31063770 | https://www.ncbi.nlm.nih.gov/pubmed/26689774

Cenobamate (also known as YKP3089) is a small molecule sodium channel blocker in development for the treatment of partial-onset seizures in adult patients. In mice and rats, Cenobamate displayed an anticonvulsant activity in the maximal electroshock test and prevented seizures induced by chemical convulsants such as pentylenetetrazol and picrotoxin. In addition, Cenobamate was reported to be effective in two models of focal seizure, the hippocampal kindled rat and the mouse 6 Hz psychomotor seizure models. Two completed adequate and well-controlled clinical studies demonstrated a significant reduction in focal seizures with Cenobamate in patients with epilepsy, and a long-term open-label phase 3 safety clinical trial is currently ongoing. Cenobamate is considered a new generation antiepileptic therapy and clinical trials have shown that it may be more effective and safer than existing drugs. If licensed, Cenobamate will offer a new adjunctive treatment option for patients with partial focal epilepsy.

Originator

Approval Year

C_max

Value	Dose	Analyte	Population
24.1 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32087001/	200 mg 1 times / day steady-state, oral dose: 200 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	CENOBAMATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
46.1 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32087001/	400 mg 1 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	CENOBAMATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
17.2 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32087001/	750 mg single, oral dose: 750 mg route of administration: Oral experiment type: SINGLE co-administered:	CENOBAMATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
4.42 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32087001/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	CENOBAMATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
0.1 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32087001/	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	CENOBAMATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
484 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32087001/	200 mg 1 times / day steady-state, oral dose: 200 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	CENOBAMATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
873 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32087001/	400 mg 1 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	CENOBAMATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1960 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32087001/	750 mg single, oral dose: 750 mg route of administration: Oral experiment type: SINGLE co-administered:	CENOBAMATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
322 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32087001/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	CENOBAMATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
4.53 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32087001/	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	CENOBAMATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
482 μg × h/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf	200 mg 1 times / day steady-state, oral dose: 200 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	CENOBAMATE unknown	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
861 μg × h/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf	400 mg 1 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	CENOBAMATE unknown	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
75.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32087001/	750 mg single, oral dose: 750 mg route of administration: Oral experiment type: SINGLE co-administered:	CENOBAMATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
54.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32087001/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	CENOBAMATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
35.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32087001/	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	CENOBAMATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
40% OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf	200 mg 1 times / day steady-state, oral dose: 200 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		CENOBAMATE unknown	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
40% OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf	400 mg 1 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		CENOBAMATE unknown	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
200 mg 1 times / day steady, oral Recommended Dose: 200 mg, 1 times / day Route: oral Route: steady Dose: 200 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/32409485/	unhealthy, 18 to 65 years n = 113 Health Status: unhealthy Condition: partial-onset seizures Age Group: 18 to 65 years Sex: M+F Population Size: 113 Sources: https://pubmed.ncbi.nlm.nih.gov/32409485/	Disc. AE: Tachycardia, Gastroesophageal reflux disease... Other AEs: Somnolence, Dizziness... AEs leading to discontinuation/dose reduction: Tachycardia Gastroesophageal reflux disease Drug hypersensitivity Nystagmus Aggression Depression Dyspnea Other AEs: Somnolence (grade 1-2, 22.1%) Dizziness (grade 1-2, 22.1%) Headache (grade 1-2, 12.4%) Nausea (grade 1-2, 11.5%) Fatigue (grade 1-2, 10.6%) Nystagmus (grade 1-2, 9.7%) Balance disorder (grade 1-2, 8%) Urinary tract infection (grade 1-2, 8%) Upper respiratory tract infection (grade 1-2, 7.1%) Tremor (grade 1-2, 6.2%) Nasopharyngitis (grade 1-2, 6.2%) Constipation (grade 1-2, 5.3%) Diarrhea (grade 1-2, 5.3%) Vomiting (grade 1-2, 5.3%) Anxiety (grade 1-2, 0.9%) Sources: https://pubmed.ncbi.nlm.nih.gov/32409485/
100 mg 1 times / day steady, oral Recommended Dose: 100 mg, 1 times / day Route: oral Route: steady Dose: 100 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212839s000lbl.pdf	unhealthy, mean age 39 years n = 108 Health Status: unhealthy Condition: partial-onset seizures Age Group: mean age 39 years Sex: M+F Population Size: 108 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212839s000lbl.pdf	Other AEs: Vertigo, Diplopia... Other AEs: Vertigo (1%) Diplopia (6%) Vision blurred (2%) Nausea (6%) Constipation (2%) Diarrhea (1%) Vomiting (2%) Dry mouth (1%) Abdominal pain (2%) Dyspepsia (2%) Nasopharyngitis (2%) Pharyngitis (1%) Urinary tract infection (2%) Head injury (1%) Alanine aminotransferase increased (1%) Aspartate aminotransferase increased (1%) Weight decreased (2%) Decreased appetite (3%) Back pain (4%) Musculoskeletal chest pain (2%) Somnolence (19%) Dizziness (18%) Fatigue (12%) Headache (10%) Balance disorder (3%) Gait disturbance (1%) Dysarthria (2%) Nystagmus (3%) Ataxia (2%) Aphasia (2%) Dysgeusia (2%) Memory impairment (2%) Sedation (1%) Confusional state (2%) Irritability (1%) Suicidal ideation (2%) Dysmenorrhea (1%) Pruritus (2%) Rash papular (2%) ALT increased (0.9%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212839s000lbl.pdf
200 mg 1 times / day steady, oral Recommended Dose: 200 mg, 1 times / day Route: oral Route: steady Dose: 200 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212839s000lbl.pdf	unhealthy, mean age 39 years n = 109 Health Status: unhealthy Condition: partial-onset seizures Age Group: mean age 39 years Sex: M+F Population Size: 109 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212839s000lbl.pdf	Other AEs: ALT increased... Other AEs: ALT increased (1.8%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212839s000lbl.pdf
200 mg 1 times / day steady, oral Recommended Dose: 200 mg, 1 times / day Route: oral Route: steady Dose: 200 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212839s000lbl.pdf	unhealthy, mean age 39 years n = 223 Health Status: unhealthy Condition: partial-onset seizures Age Group: mean age 39 years Sex: M+F Population Size: 223 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212839s000lbl.pdf	Other AEs: Vertigo, Diplopia... Other AEs: Vertigo (1%) Diplopia (7%) Vision blurred (2%) Nausea (6%) Constipation (4%) Diarrhea (3%) Vomiting (4%) Dry mouth (1%) Abdominal pain (2%) Dyspepsia (2%) Nasopharyngitis (4%) Pharyngitis (2%) Urinary tract infection (5%) Alanine aminotransferase increased (1%) Aspartate aminotransferase increased (1%) Decreased appetite (1%) Back pain (2%) Musculoskeletal chest pain (1%) Somnolence (22%) Dizziness (22%) Fatigue (14%) Headache (12%) Balance disorder (5%) Gait disturbance (3%) Dysarthria (1%) Nystagmus (7%) Ataxia (3%) Aphasia (1%) Memory impairment (1%) Sedation (1%) Confusional state (2%) Suicidal ideation (1%) Dysmenorrhea (2%) Pruritus (1%) Asthenia (1%) Tremor (3%) Pollakiuria (1%) Hiccups (1%) Dyspnea (3%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212839s000lbl.pdf
350 mg 1 times / day steady, oral (mean) Recommended Dose: 350 mg, 1 times / day Route: oral Route: steady Dose: 350 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212839s000lbl.pdf	unhealthy, mean age 39 years n = 442 Health Status: unhealthy Condition: partial-onset seizures Age Group: mean age 39 years Sex: M+F Population Size: 442 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212839s000lbl.pdf	Disc. AE: Ataxia, Dizziness... AEs leading to discontinuation/dose reduction: Ataxia (>1) Dizziness (>1) Somnolence (>1) Diplopia (>1) Nystagmus (>1) Vertigo (>1) Cognitive deterioration (0.4%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212839s000lbl.pdf
400 mg 1 times / day steady, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212839s000lbl.pdf	unhealthy, mean age 39 years n = 111 Health Status: unhealthy Condition: partial-onset seizures Age Group: mean age 39 years Sex: M+F Population Size: 111 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212839s000lbl.pdf	Other AEs: Nystagmus, Ataxia... Other AEs: Nystagmus (6%) Ataxia (6%) Aphasia (4%) Asthenia (3%) Vertigo (6%) Diplopia (15%) Palpitations (2%) Vision blurred (4%) Nausea (9%) Constipation (8%) Diarrhea (5%) Vomiting (5%) Dry mouth (3%) Abdominal pain (1%) Nasopharyngitis (5%) Head injury (2%) Alanine aminotransferase increased (4%) Aspartate aminotransferase increased (3%) Weight decreased (1%) Decreased appetite (5%) Back pain (5%) Somnolence (37%) Dizziness (33%) Fatigue (24%) Headache (10%) Balance disorder (9%) Gait disturbance (8%) Dysarthria (7%) Dysgeusia (2%) Memory impairment (2%) Migraine (2%) Sedation (2%) Tremor (1%) Confusional state (3%) Euphoric mood (2%) Irritability (2%) Dysmenorrhea (1%) Hiccups (1%) ALT increased (2.7%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212839s000lbl.pdf
750 mg 1 times / day single, oral Highest studied dose Dose: 750 mg, 1 times / day Route: oral Route: single Dose: 750 mg, 1 times / day Sources: http://az9194.vo.msecnd.net/pdfs/110404/11.08.pdf https://pubmed.ncbi.nlm.nih.gov/32087001/	healthy n = 7 Health Status: healthy Sex: M Population Size: 7 Sources: http://az9194.vo.msecnd.net/pdfs/110404/11.08.pdf https://pubmed.ncbi.nlm.nih.gov/32087001/	Other AEs: Nervous system disorders... Other AEs: Nervous system disorders (71.4%) Sources: http://az9194.vo.msecnd.net/pdfs/110404/11.08.pdf https://pubmed.ncbi.nlm.nih.gov/32087001/

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inducer 781	inhibitor 1767 inducer 389	inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2B6 810 CYP2C19 1478 CYP3A4/5 278 CYP1A2 1524 CYP2C8 911 P-gp 1461 OAT1 599 OCT1 512 OCT2 647 OATP1B3 706 BSEP 402 OAT3 642 OATP1B1 788	UGT2B7 389 UGT2B4 249 CYP2E1 667 CYP2A6 543 CYP2B6 664 CYP2C19 991 CYP3A4/5 85 P-gp 1537 BCRP 561 OAT1 326 OAT3 339 OCT2 355 MATE1 135 MATE2 96	CYP2B6 547 CYP2C8 168 CYP1A2 701 CYP2C19 293

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
BSEP 403	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	no
CYP1A2 1692	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	no
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	no
CYP2C19 1553	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	no
CYP2C8 965	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	no
CYP2C9 1819	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	no
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	no
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	no
OAT1 603	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	no
OATP1B3 715	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	no
OCT1 543	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	no
OCT2 648	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	no
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	no
OAT3 644	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	weak
OATP1B1 803	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	weak
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	yes [IC50 170 uM]	yes (co-administration study) Comment: Cenobamate increases exposure of phenytoin, omeprazole (CYP2C19 probe substrate) by approximately 2-fold when administered concomitantly Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0
CYP2B6 1001	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	yes [IC50 280 uM]
CYP3A4/5 335	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	yes [IC50 720 uM]
CYP2B6 1001	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	yes
CYP2C8 965	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	yes
CYP3A4 1925	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	yes	yes (co-administration study) Comment: Cendobamate decreases midazolam concentration upto 4-fold (CYP3A induction) when administered concomitantly. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0

Drug as victim

Target	Modality	Activity
UGT2B7 389	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	major
BCRP 561	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	no
MATE1 135	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	no
MATE2 96	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	no
OAT1 326	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	no
OAT3 339	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	no
OCT2 355	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	no
P-gp 1537	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	no
CYP2A6 543	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	yes
CYP2B6 664	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	yes
CYP2C19 991	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	yes
CYP2E1 667	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	yes
CYP3A4/5 85	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	yes
UGT2B4 249	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000ClinPharmR.pdf#page=11 Page: 11.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1647	inhibitor 1626 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212839Orig1s000PharmR.pdf#page=6 Page: 6.0

Sourcing

Vendor/Aggregator	ID	URL
Chem Scene	CS-0014686	http://www.chemscene.com/913088-80-9.html
DC Chemicals	Cenobamate	http://www.dcchemicals.com/product_show-DC11114.html
Excenen	EX-A3604	https://www.excenen.com/searchresultlist.php?id=EX-A3604
Hairui	CECQ033	http://www.hairuichem.com/en/product/913088-80-9.html
MedChem Express	HY-17607	https://www.medchemexpress.com/Cenobamate.html
MolPort	MolPort-047-786-375	https://www.molport.com/shop/molecule-link/MolPort-047-786-375
Molnova	M16559
THE BioTek	bt-506132	https://www.thebiotek.com/product/others/bt-506132
ZINC	ZINC000116846024	http://zinc15.docking.org/substances/ZINC000116846024
eNovation Chemicals	D673497	https://www.enovationchem.com/ProductDetails.asp?ProductID=D673497

PubMed

Title	Date	PubMed
Antiepileptic Drugs in Clinical Development: Differentiate or Die?	2017	28799516

Patents

Sample Use Guides

In Vivo Use Guide

target dose of 200 mg/day

Route of Administration: Oral

Name

Type

Language

CENOBAMATE

Official Name

English

2H-TETRAZOLE-2-ETHANOL, .ALPHA.-(2-CHLOROPHENYL)-, CARBAMATE (ESTER), (.ALPHA.R)-

Systematic Name

English

YKP-3089

Code

English

CARBAMIC ACID (R)-(+)-1-(2-CHLOROPHENYL)-2-(2H-TETRAZOL-2-YL)ETHYL ESTER

Systematic Name

English

cenobamate [INN]

Common Name

English

XCOPRI

Brand Name

English

2H-TETRAZOLE-2-ETHANOL, .ALPHA.-(2-CHLOROPHENYL)-, 2-CARBAMATE, (.ALPHA.R)-

Systematic Name

English

2H-TETRAZOLE-2-ETHANOL, ALPHA-(2-CHLOROPHENYL)-, YL)ETHYL)CARBAMATE CARBAMATE (ESTER), (.ALPHA.R)-

Systematic Name

English

CENOBAMATE [ORANGE BOOK]

Common Name

English

CENOBAMATE [USAN]

Common Name

English

(1R)-1-(2-CHLOROPHENYL)-2-(TETRAZOL-YL)ETHYL)CARBAMATE

Common Name

English

YKP3089

Code

English

(1R)-1-(2-Chlorophenyl)-2-(2H-tetrazol-2-yl)ethyl carbamate

Systematic Name

English

Cenobamate [WHO-DD]

Common Name

English

CENOBAMATE [MI]

Common Name

English

Classification Tree Code System Code

DEA NO.

2720