OMIDENEPAG

US Previously Marketed

Details

Stereochemistry	ACHIRAL
Molecular Formula	C23H22N6O4S
Molecular Weight	478.524
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC(=O)CNC1=CC=CC(CN(CC2=CC=C(C=C2)N3C=CC=N3)S(=O)(=O)C4=CC=CN=C4)=N1

InChI

InChIKey=YHGSTSNEOJUIRN-UHFFFAOYSA-N

InChI=1S/C23H22N6O4S/c30-23(31)15-25-22-6-1-4-19(27-22)17-28(34(32,33)21-5-2-11-24-14-21)16-18-7-9-20(10-8-18)29-13-3-12-26-29/h1-14H,15-17H2,(H,25,27)(H,30,31)

HIDE SMILES / InChI

Description
Sources: https://pubmed.ncbi.nlm.nih.gov/30465134|https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/215092s000lbl.pdf

Omidenepag isopropyl, a prodrug, is hydrolyzed in the eye to the active form (Omidenepag) which functions as a selective, nonprostaglandin, prostanoid EP2 agonist, has been developed by Ube Industries and Santen Pharmaceutical as an ophthalmic solution (EYBELIS®) for the treatment of glaucoma and ocular hypertension. Omidenepag isopropyl increases the outfow of aqueous humor via both the uveoscleral outfow and the trabecular outfow pathways, resulting in potent and stable reduction in intraocular pressure (IOP). In September 2018, omidenepag isopropyl ophthalmic solution 0.002% was approved in Japan for the treatment of glaucoma and ocular hypertension. On September 22, 2022, the FDA approved Santen’s Omlonti (omidenepag isopropyl), for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension.

Approval Year

Conditions

Condition	Modality	Targets	Highest Phase	Product
Open-angle glaucoma 53 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/215092s000lbl.pdf	Primary		Approved 8583	Omlonti Approved Use Omlonti (omidenepag isopropyl ophthalmic solution) 0.002%, is a relatively selective prostaglandin E2 (EP2) receptor agonist, indicated for the reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension. Launch Date 2022
Ocular hypertension 52 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/215092s000lbl.pdf	Primary		Approved 8583	Omlonti Approved Use Omlonti (omidenepag isopropyl ophthalmic solution) 0.002%, is a relatively selective prostaglandin E2 (EP2) receptor agonist, indicated for the reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension. Launch Date 2022

C_max

Value	Dose	Co-administered	Analyte	Population
34.36 pg/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf#page=7 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf#page=15 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf#page=21	1 drop 1 times / day multiple, ocular dose: 1 drop route of administration: Ocular experiment type: MULTIPLE co-administered:		OMIDENEPAG ISOPROPYL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
21.54 pmol × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf#page=7 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf#page=15 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf#page=21	1 drop 1 times / day multiple, ocular dose: 1 drop route of administration: Ocular experiment type: MULTIPLE co-administered:		OMIDENEPAG ISOPROPYL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
0.449 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf#page=7 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf#page=15 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf#page=21	1 drop 1 times / day multiple, ocular dose: 1 drop route of administration: Ocular experiment type: MULTIPLE co-administered:		OMIDENEPAG ISOPROPYL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
2.2% OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf#page=7 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf#page=15 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf#page=21	1 drop 1 times / day multiple, ocular dose: 1 drop route of administration: Ocular experiment type: MULTIPLE co-administered:		OMIDENEPAG ISOPROPYL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
0.002 % 1 times / day steady, ophthalmic Studied dose Dose: 0.002 %, 1 times / day Route: ophthalmic Route: steady Dose: 0.002 %, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000MedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000MedR.pdf	Disc. AE: Photophobia, Uveitis... AEs leading to discontinuation/dose reduction: Photophobia (1 patient) Uveitis (1 patient) Iritis (1 patient) Foreign body (1 patient) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000MedR.pdf
0.002 % 1 times / day steady, ophthalmic Studied dose Dose: 0.002 %, 1 times / day Route: ophthalmic Route: steady Dose: 0.002 %, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000SumR.pdf	unhealthy Health Status: unhealthy Sex: unknown Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000SumR.pdf	Other AEs: Conjunctival hyperemia, Photophobia... Other AEs: Conjunctival hyperemia (9.7%) Photophobia (3.2%) Ocular hyperemia (1.6%) Vision blurred (1.1%) Eye pain (1.6%) Corneal thickening (3.8%) Dry eye (1.1%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000SumR.pdf

AEs

AE	Significance	Dose	Population
Foreign body	1 patient Disc. AE	0.002 % 1 times / day steady, ophthalmic Studied dose Dose: 0.002 %, 1 times / day Route: ophthalmic Route: steady Dose: 0.002 %, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000MedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000MedR.pdf
Iritis	1 patient Disc. AE	0.002 % 1 times / day steady, ophthalmic Studied dose Dose: 0.002 %, 1 times / day Route: ophthalmic Route: steady Dose: 0.002 %, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000MedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000MedR.pdf
Photophobia	1 patient Disc. AE	0.002 % 1 times / day steady, ophthalmic Studied dose Dose: 0.002 %, 1 times / day Route: ophthalmic Route: steady Dose: 0.002 %, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000MedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000MedR.pdf
Uveitis	1 patient Disc. AE	0.002 % 1 times / day steady, ophthalmic Studied dose Dose: 0.002 %, 1 times / day Route: ophthalmic Route: steady Dose: 0.002 %, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000MedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000MedR.pdf
Dry eye	1.1%	0.002 % 1 times / day steady, ophthalmic Studied dose Dose: 0.002 %, 1 times / day Route: ophthalmic Route: steady Dose: 0.002 %, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000SumR.pdf	unhealthy Health Status: unhealthy Sex: unknown Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000SumR.pdf
Vision blurred	1.1%	0.002 % 1 times / day steady, ophthalmic Studied dose Dose: 0.002 %, 1 times / day Route: ophthalmic Route: steady Dose: 0.002 %, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000SumR.pdf	unhealthy Health Status: unhealthy Sex: unknown Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000SumR.pdf
Eye pain	1.6%	0.002 % 1 times / day steady, ophthalmic Studied dose Dose: 0.002 %, 1 times / day Route: ophthalmic Route: steady Dose: 0.002 %, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000SumR.pdf	unhealthy Health Status: unhealthy Sex: unknown Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000SumR.pdf
Ocular hyperemia	1.6%	0.002 % 1 times / day steady, ophthalmic Studied dose Dose: 0.002 %, 1 times / day Route: ophthalmic Route: steady Dose: 0.002 %, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000SumR.pdf	unhealthy Health Status: unhealthy Sex: unknown Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000SumR.pdf
Photophobia	3.2%	0.002 % 1 times / day steady, ophthalmic Studied dose Dose: 0.002 %, 1 times / day Route: ophthalmic Route: steady Dose: 0.002 %, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000SumR.pdf	unhealthy Health Status: unhealthy Sex: unknown Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000SumR.pdf
Corneal thickening	3.8%	0.002 % 1 times / day steady, ophthalmic Studied dose Dose: 0.002 %, 1 times / day Route: ophthalmic Route: steady Dose: 0.002 %, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000SumR.pdf	unhealthy Health Status: unhealthy Sex: unknown Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000SumR.pdf
Conjunctival hyperemia	9.7%	0.002 % 1 times / day steady, ophthalmic Studied dose Dose: 0.002 %, 1 times / day Route: ophthalmic Route: steady Dose: 0.002 %, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000SumR.pdf	unhealthy Health Status: unhealthy Sex: unknown Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000SumR.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946	substrate 1193 inhibitor 2438	inhibitor 2507 substrate 1388	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
OATP1B1 1079 BCRP 910 OAT3 747 MATE1 415 MATE2-K 77 OATP1B3 961 OAT1 725 OCT1 620 P-gp 1741 BSEP 550 OCT2 779 CYP3A4/5 296 CYP2C19 2057 CYP1A2 2153 CYP2B6 926 CYP2C8 1057	OCT2 434 OATP1B3 435 MATE1 182 MATE2-K 33 OAT1 395 OATP1B1 503 OAT3 391 BCRP 697 P-gp 2052 OCT1 393 BSEP 63 CES2 33 CYP2B6 776 CES1 45 CYP1A2 1197 CYP2A6 626 CYP2C8 810 CYP2C19 1119 CYP2E1 729

Drug as perpetrator

Target	Modality	Activity	Metabolite
BCRP 985	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 11	no
BCRP 985	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 11	no	OMIDENEPAG 2
BSEP 554	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 11	no	OMIDENEPAG 2
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 26 \| 11	no	OMIDENEPAG 2
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 26 \| 11	no	OMIDENEPAG 2
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 26 \| 11	no	OMIDENEPAG 2
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 26 \| 11	no	OMIDENEPAG 2
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 26 \| 11	no	OMIDENEPAG 2
MATE1 416	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 11	no	OMIDENEPAG 2
OAT1 730	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 11	no
OAT1 730	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 11	no	OMIDENEPAG 2
OCT1 656	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 11	no	OMIDENEPAG 2
OCT2 782	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 11	no
OCT2 782	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 11	no	OMIDENEPAG 2
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 11	no
BSEP 554	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 11	weak [IC50 >5 uM]
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 11	weak [IC50 >5 uM]	OMIDENEPAG 2
OATP1B1 1095	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 11	yes [IC50 1.8 uM]	OMIDENEPAG 2
OATP1B1 1095	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 11	yes [IC50 1.89 uM]
OCT1 656	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 11	yes [IC50 2.26 uM]
CYP3A4/5 357	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 26 \| 11	yes [IC50 5.04 uM]	OMIDENEPAG 2
OAT3 749	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 11	yes [IC50 7.13 uM]	OMIDENEPAG 2
OAT3 749	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 11	yes [IC50 8.96 uM]
MATE2-K 77	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 11	yes [IC50 <=5 uM]
MATE1 416	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 11	yes [IC50 >5 uM]
MATE2-K 77	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 11	yes [IC50 >5 uM]	OMIDENEPAG 2
OATP1B3 970	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 11	yes [IC50 >5 uM]
OATP1B3 970	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 11	yes [IC50 >5 uM]	OMIDENEPAG 2
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 26 \| 11	yes	OMIDENEPAG 2

Drug as victim

Target	Modality	Activity	Metabolite
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 25.0	major	OMIDENEPAG 2
CYP1A2 1197	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 25.0	minor	OMIDENEPAG 2
CYP2A6 626	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 25.0	minor	OMIDENEPAG 2
CYP2B6 776	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 25.0	minor	OMIDENEPAG 2
CYP2C19 1119	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 25.0	minor	OMIDENEPAG 2
CYP2C8 810	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 25.0	minor	OMIDENEPAG 2
CYP2C9 1193	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 25.0	minor	OMIDENEPAG 2
CYP2D6 1388	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 25.0	minor	OMIDENEPAG 2
CYP2E1 729	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 25.0	minor	OMIDENEPAG 2
BCRP 697	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 10	no
BCRP 697	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 10	no	OMIDENEPAG 2
BSEP 63	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 10	no
BSEP 63	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 10	no	OMIDENEPAG 2
CES2 33	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 24.0	no
MATE1 182	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 10	no
MATE1 182	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 10	no	OMIDENEPAG 2
MATE2-K 33	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 10	no
MATE2-K 33	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 10	no	OMIDENEPAG 2
OAT1 395	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 10	no
OAT1 395	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 10	no	OMIDENEPAG 2
OAT3 391	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 10	no
OATP1B1 503	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 10	no
OATP1B3 435	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 10	no
OCT1 393	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 10	no
OCT1 393	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 10	no	OMIDENEPAG 2
OCT2 434	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 10	no
OCT2 434	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 10	no	OMIDENEPAG 2
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 10	no
CES1 45	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 24.0	yes
OAT3 391	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 10	yes	OMIDENEPAG 2
OATP1B1 503	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 10	yes	OMIDENEPAG 2
OATP1B3 435	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 10	yes	OMIDENEPAG 2
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 28 \| 10	yes	OMIDENEPAG 2

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215092Orig1s000ClinPharmR.pdf Page: 10.0		OMIDENEPAG 2

PubMed

Title	Date	PubMed
Omidenepag Isopropyl Versus Latanoprost in Primary Open-Angle Glaucoma and Ocular Hypertension: The Phase 3 AYAME Study.	2020-12	32533949
Omidenepag isopropyl for the treatment of glaucoma and ocular hypertension.	2019-06	31250842
Omidenepag Isopropyl Ophthalmic Solution 0.002%: First Global Approval.	2018-12	30465134
Omidenepag Isopropyl Ophthalmic Solution 0.002%: First Global Approval.	2018-12	30465134

Patents

Sample Use Guides

In Vivo Use Guide

Ophthalmic solution containing 0.002% (0.02 mg/mL) of omidenepag isopropyl. The recommended dosage is one drop in the affected eye(s) once daily in the evening.

Route of Administration: Topical

Name

Type

Language

OMIDENEPAG

Official Name

English

UR-7276

Preferred Name

English

GLYCINE, N-(6-((((4-(1H-PYRAZOL-1-YL)PHENYL)METHYL)(3-PYRIDINYLSULFONYL)AMINO)METHYL)-2-PYRIDINYL)-

Systematic Name

English

((6-(((4-(PYRAZOL-1-YL)BENZYL)(PYRIDIN-3-YLSULFONYL)AMINO)METHYL)PYRIDIN-2-YL)AMINO)ACETIC ACID

Systematic Name

English

((6-((N-((4-(1H-PYRAZOL-1-YL)PHENYL)METHYL)PYRIDINE-3-SULFONAMIDO)METHYL)PYRIDIN-2-YL)AMINO)ACETIC ACID

Systematic Name

English

omidenepag [INN]

Common Name

English

Omidenepag [WHO-DD]

Common Name

English

OMIDENEPAG [USAN]

Common Name

English

Classification Tree Code System Code

WHO-ATC

S01EX06