DARIDOREXANT

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C23H23ClN6O2
Molecular Weight	450.921
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COC1=CC(C(=O)N2CCC[C@@]2(C)C3=NC4=C(N3)C=CC(Cl)=C4C)=C(C=C1)N5N=CC=N5

InChI

InChIKey=NBGABHGMJVIVBW-QHCPKHFHSA-N

InChI=1S/C23H23ClN6O2/c1-14-17(24)6-7-18-20(14)28-22(27-18)23(2)9-4-12-29(23)21(31)16-13-15(32-3)5-8-19(16)30-25-10-11-26-30/h5-8,10-11,13H,4,9,12H2,1-3H3,(H,27,28)/t23-/m0/s1

HIDE SMILES / InChI

Molecular Formula	C23H23ClN6O2
Molecular Weight	450.921
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://pubmed.ncbi.nlm.nih.gov/35298826|https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/214985s000lbl.pdf

Daridorexant (Quviviq™; Idorsia Pharmaceuticals Ltd.) is an orally administered dual orexin type 1 and type 2 (OX1 and OX2) receptor antagonist (DORA) being developed for the treatment of insomnia. It was selected from a pool of drug candidates on the basis of an expected effect duration of ≈ 8 h at a dose of 25 mg, with a half-life intended to minimize residual effects that might impair daytime functioning. Based on the results of two pivotal phase III trials, daridorexant was recently approved in the USA for the treatment of adult patients with insomnia characterized by difficulties with sleep onset and/or sleep maintenance. The mechanism of action of daridorexant in the treatment of insomnia is presumed to be through antagonism of orexin receptors. The orexin neuropeptide signaling system plays a role in wakefulness. Blocking the binding of wake-promoting neuropeptides orexin A and orexin B to receptors OX1R and OX2R is thought to suppress wake drive.

CNS Activity

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Orexin receptor 1 8 Target ID: CHEMBL5113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/214985s000lbl.pdf	Antagonist 2849		8.8 null [pKi]
Orexin receptor 2 10 Target ID: CHEMBL4792 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/214985s000lbl.pdf	Antagonist 2849		8.9 null [pKi]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Insomnia 111 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/214985s000lbl.pdf	Primary		Approved 8583	QUVIVIQ Approved Use Indicated for the treatment of adult patients with insomnia characterized by difficulties with sleep onset and/or sleep maintenance. Launch Date 2022

C_max

Value	Dose	Analyte	Population
954.68 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=44 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=45	50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DARIDOREXANT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
160 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=234	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
632 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=234	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1231 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=234	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1557 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=234	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1869 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=234	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
256 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=235	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
280 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=235	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
614 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=235	25 mg 1 times / day multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
616 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=235	25 mg 1 times / day multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1225 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=235	75 mg 1 times / day multiple, oral dose: 75 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1308 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=235	75 mg 1 times / day multiple, oral dose: 75 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
9981.47 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=44 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=45	50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DARIDOREXANT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
894 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=234	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2568 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=234	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
6947 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=234	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
10998 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=234	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
17864 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=234	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1156 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=235	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1293 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=235	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3502 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=235	25 mg 1 times / day multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3805 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=235	25 mg 1 times / day multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
8583 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=235	75 mg 1 times / day multiple, oral dose: 75 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
8940 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=235	75 mg 1 times / day multiple, oral dose: 75 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
8 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=44 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=45	50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DARIDOREXANT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
6.5 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=234	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
6.1 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=234	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
5.9 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=234	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
7.5 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=234	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
8.8 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=234	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
5.9 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=235	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
5.6 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=235	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
5.9 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=235	25 mg 1 times / day multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
6.7 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=235	25 mg 1 times / day multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
9.2 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=235	75 mg 1 times / day multiple, oral dose: 75 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
8.5 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=235	75 mg 1 times / day multiple, oral dose: 75 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DARIDOREXANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
0.3% OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=45 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=169			DARIDOREXANT plasma	Homo sapiens

Doses

Dose	Population	Adverse events
50 mg 1 times / day steady, oral Recommended\|Highest studied dose Dose: 50 mg, 1 times / day Route: oral Route: steady Dose: 50 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000RiskR.pdf	unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000RiskR.pdf	Disc. AE: Supraventricular extrasystoles, Renal Impairment... AEs leading to discontinuation/dose reduction: Supraventricular extrasystoles (1 patient) Renal Impairment (1 patient) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000RiskR.pdf
25 mg 1 times / day steady, oral Recommended\|Studied dose Dose: 25 mg, 1 times / day Route: oral Route: steady Dose: 25 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000RiskR.pdf	unhealthy Health Status: unhealthy Sex: M F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000RiskR.pdf	Disc. AE: colitis ulcerative, sedation... AEs leading to discontinuation/dose reduction: colitis ulcerative (1 patient) sedation (1 patient) dizziness (2 patients) poor quality sleep (1 patient) sleep paralysis (1 patient) depressed mood (1 patient) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000RiskR.pdf

AEs

AE	Significance	Dose	Population
Renal Impairment	1 patient Disc. AE	50 mg 1 times / day steady, oral Recommended\|Highest studied dose Dose: 50 mg, 1 times / day Route: oral Route: steady Dose: 50 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000RiskR.pdf	unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000RiskR.pdf
Supraventricular extrasystoles	1 patient Disc. AE	50 mg 1 times / day steady, oral Recommended\|Highest studied dose Dose: 50 mg, 1 times / day Route: oral Route: steady Dose: 50 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000RiskR.pdf	unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000RiskR.pdf
colitis ulcerative	1 patient Disc. AE	25 mg 1 times / day steady, oral Recommended\|Studied dose Dose: 25 mg, 1 times / day Route: oral Route: steady Dose: 25 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000RiskR.pdf	unhealthy Health Status: unhealthy Sex: M F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000RiskR.pdf
depressed mood	1 patient Disc. AE	25 mg 1 times / day steady, oral Recommended\|Studied dose Dose: 25 mg, 1 times / day Route: oral Route: steady Dose: 25 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000RiskR.pdf	unhealthy Health Status: unhealthy Sex: M F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000RiskR.pdf
poor quality sleep	1 patient Disc. AE	25 mg 1 times / day steady, oral Recommended\|Studied dose Dose: 25 mg, 1 times / day Route: oral Route: steady Dose: 25 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000RiskR.pdf	unhealthy Health Status: unhealthy Sex: M F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000RiskR.pdf
sedation	1 patient Disc. AE	25 mg 1 times / day steady, oral Recommended\|Studied dose Dose: 25 mg, 1 times / day Route: oral Route: steady Dose: 25 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000RiskR.pdf	unhealthy Health Status: unhealthy Sex: M F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000RiskR.pdf
sleep paralysis	1 patient Disc. AE	25 mg 1 times / day steady, oral Recommended\|Studied dose Dose: 25 mg, 1 times / day Route: oral Route: steady Dose: 25 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000RiskR.pdf	unhealthy Health Status: unhealthy Sex: M F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000RiskR.pdf
dizziness	2 patients Disc. AE	25 mg 1 times / day steady, oral Recommended\|Studied dose Dose: 25 mg, 1 times / day Route: oral Route: steady Dose: 25 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000RiskR.pdf	unhealthy Health Status: unhealthy Sex: M F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000RiskR.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946 inhibitor 2252 inducer 1087	inhibitor 2438 substrate 1193 inducer 440	inhibitor 2507 substrate 1388	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2C19 2057 CYP1A2 2153 CYP2C8 1057 CYP2B6 926 CYP2A6 879 MATE2-K 77 MATE1 415 OATP1B1 1079 OATP1B3 961 OAT3 747 P-gp 1741 OCT1 620 BCRP 910	OATP1B3 435 P-gp 2052 CYP1A2 1197 CYP2C8 810 CYP2C19 1119 BCRP 697 OATP1B1 503	CYP1A2 832 CYP2B6 669

Drug as perpetrator

Target	Modality	Activity	Metabolite	Clinical evidence
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=172 Page: 172.0	no [IC50 >44 uM]	M1 13
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=172 Page: 172.0	no [IC50 >44 uM]	M1 13
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=172 Page: 172.0	no [IC50 >44 uM]	M1 13
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=172 Page: 172.0	no [IC50 >=50 uM]
CYP2A6 911	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=172 Page: 172.0	no [IC50 >=50 uM]
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=172 Page: 172.0	no [IC50 >=50 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=172 Page: 172.0	no [IC50 >=50 uM]
BCRP 985	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=173 Page: 173 \| 232 \| 46	weak [IC50 3 uM]		no (co-administration study) Comment: Unchanged rosuvastatin Cmax and AUCinf (both 0.93-fold) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=173 Page: 173 \| 232 \| 46
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=172 Page: 172 \| 230 \| 46 \| 249	weak [IC50 7.3 uM]		yes (co-administration study) Comment: Slightly increased midazolam Cmax and AUC24 by 1.2-fold and 1.11-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=172 Page: 172 \| 230 \| 46 \| 249
PXR 51	activator 342 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=46 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=172 Page: 46 \| 172	yes [EC50 3 uM]
OCT1 656	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=173 Page: 173.0	yes [IC50 0.5 uM]	M1 13
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=172 Page: 172.0	yes [IC50 11 uM]	M1 13
OATP1B1 1095	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=173 Page: 173 \| 232	yes [IC50 11 uM]
MATE1 416	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=173 Page: 173.0	yes [IC50 16 uM]	M1 13
OATP1B3 970	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=173 Page: 173 \| 232	yes [IC50 16 uM]
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=172 Page: 172.0	yes [IC50 17 uM]	M1 13
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=172 Page: 172.0	yes [IC50 18 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=172 Page: 172.0	yes [IC50 19 uM]
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=173 Page: 173 \| 232	yes [IC50 24 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=172 Page: 172.0	yes [IC50 26 uM]	M1 13
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=172 Page: 172.0	yes [IC50 26 uM]	M1 13
BCRP 985	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=173 Page: 173.0	yes [IC50 31 uM]	M1 13
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=173 Page: 173.0	yes [IC50 31 uM]	M1 13
OAT3 749	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=173 Page: 173 \| 232	yes [IC50 39 uM]
OATP1B1 1095	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=173 Page: 173.0	yes [IC50 4.5 uM]	M1 13
OCT1 656	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=173 Page: 173 \| 232	yes [IC50 71 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=172 Page: 172 \| 211	yes [IC50 8.2 uM]
MATE2-K 77	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=173 Page: 173 \| 232	yes [IC50 8.4 uM]
MATE1 416	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=173 Page: 173 \| 232	yes [IC50 9.7 uM]
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=231 Page: 231.0	yes
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=173 Page: 173.0	yes
CYP2C9 2497	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=173 Page: 173.0	yes
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=173 Page: 173.0	yes

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=45 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=153 Page: 45 \| 153 \| 170 \| 245	major	yes (co-administration study) Comment: Diltiazem increased daridorexant AUC and Cmax by 2.4 times and 1.4 times. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=45 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=153 Page: 45 \| 153 \| 170 \| 245
CYP1A2 1197	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=170 Page: 170 \| 230	minor
CYP2C19 1119	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=170 Page: 170 \| 230	minor
CYP2C8 810	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=170 Page: 170 \| 230	minor
CYP2C9 1193	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=170 Page: 170 \| 230	minor
CYP2D6 1388	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=170 Page: 170 \| 230	minor
BCRP 697	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=167 Page: 167.0	no
OATP1B1 503	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=167 Page: 167 \| 231	no
OATP1B3 435	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=167 Page: 167 \| 231	no
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=167 Page: 167.0	no

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214985Orig1s000IntegratedR.pdf#page=166 Page: 166.0

PubMed

Title	Date	PubMed
Daridorexant for the Treatment of Insomnia.	2022	36045942
Daridorexant: First Approval.	2022 Apr	35298826

Patents

Sample Use Guides

In Vivo Use Guide

The recommended dosage is 25 mg to 50 mg once per night, taken orally within 30 minutes before going to bed, with at least 7 hours remaining prior to planned awakening.

Route of Administration: Oral

In Vitro Use Guide

The Kb values were established as 1.1 nM in a rat, 0.3 nM in dog and 0.5 nM in human models with OX1r and 1.7, 0.7 and 0.8 nM for OX2r for rat, dog and human, respectively, in calcium release assays.

Substance Class	Chemical Created by `admin` on `Tue Apr 01 16:27:32 GMT 2025` Edited by `admin` on `Tue Apr 01 16:27:32 GMT 2025`
Record UNII	LMQ24G57E9
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

DARIDOREXANT

Official Name

English

ACT-541468

Preferred Name

English

(2S)-2-(5-CHLORO-4-METHYL-1H-BENZIMIDAZOL-2-YL)-2-METHYLPYRROLIDIN-1-YL)(5-METHOXY-2-(2H-1,2,3-TRIAZOL-2-YL)PHENYL)METHANONE

Systematic Name

English

DARIDOREXANT [USAN]

Common Name

English

NEMOREXANT

Common Name

English

Daridorexant [WHO-DD]

Common Name

English

(S)-2-(5-chloro-4-methyl-1H benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1-yl](5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone

Systematic Name

English

daridorexant [INN]

Common Name

English

METHANONE, ((2S)-2-(6-CHLORO-7-METHYL-1H-BENZIMIDAZOL-2-YL)-2-METHYL-1-PYRROLIDINYL)(5-METHOXY-2-(2H-1,2,3-TRIAZOL-2-YL)PHENYL)-

Systematic Name

English

DEA NO. 2410

Code

English

Classification Tree Code System Code

DEA NO.

2410