Netarsudil information

Netarsudil
Clinical data
Pronunciation	ne TAR soo dil
Trade names	Rhopressa, Rhokiinsa
Other names	AR-13324
AHFS/Drugs.com	Monograph
MedlinePlus	a618014
License data	EU EMA: by INN; US DailyMed: Netarsudil;
Routes of; administration	Eye drops, topical
ATC code	S01EX05 (WHO) ;
Legal status
Legal status	US: ℞-only; EU: Rx-only;
Pharmacokinetic data
Metabolism	Esterases in the cornea
Metabolites	AR-13503 (active metabolite)
Elimination half-life	16–17 hrs
Duration of action	≥ 24 hrs
Identifiers
	IUPAC name [4-[(2S)-3-Amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl]phenyl]methyl 2,4-dimethylbenzoate;
CAS Number	1254032-66-0;
PubChem CID	66599893;
DrugBank	DB13931;
ChemSpider	34980598;
UNII	W6I5QDT7QI;
KEGG	D11030; as salt: D11031;
CompTox Dashboard (EPA)	DTXSID001027774 ;
ECHA InfoCard	100.251.524
Chemical and physical data
Formula	C28H27N3O3
Molar mass	453.542 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES Cc1ccc(c(c1)C)C(=O)OCc2ccc(cc2)[C@@H](CN)C(=O)Nc3ccc4cnccc4c3;
	InChI InChI=1S/C28H27N3O3/c1-18-3-10-25(19(2)13-18)28(33)34-17-20-4-6-21(7-5-20)26(15-29)27(32)31-24-9-8-23-16-30-12-11-22(23)14-24/h3-14,16,26H,15,17,29H2,1-2H3,(H,31,32)/t26-/m1/s1; Key:OURRXQUGYQRVML-AREMUKBSSA-N;

Netarsudil, sold under the brand name Rhopressa among others, is a medication for the treatment of glaucoma.^[1]^[2]^[3] In the United States, in December 2017, the Food and Drug Administration (FDA) approved a 0.02% ophthalmic solution for the lowering of elevated intraocular pressure in people with open-angle glaucoma or ocular hypertension.^[4]^[5] The European Medicines Agency approved it in 2019 for the same uses under the brand name Rhokiinsa.^[2]

The FDA considers it to be a first-in-class medication.^[6]

^ ^a ^b "Rhopressa- netarsudil solution/ drops". DailyMed. Retrieved 2 May 2021.
^ ^a ^b ^c "Rhokiinsa EPAR". European Medicines Agency (EMA). 16 September 2019. Retrieved 27 September 2020.
^ Dasso L, Al-Khaled T, Sonty S, Aref AA (2018). "Profile of netarsudil ophthalmic solution and its potential in the treatment of open-angle glaucoma: evidence to date". Clinical Ophthalmology. 12. Auckland, N.Z.: 1939–1944. doi:10.2147/OPTH.S154001. PMC 6177382. PMID 30323550.
^ "Rhopressa (netarsudil) Ophthalmic Solution". U.S. Food and Drug Administration (FDA). 29 January 2018. Retrieved 3 June 2020.
^ "Aerie (AERI) Gets Early FDA Approval for Lead Drug Rhopressa". 19 December 2017.
^ New Drug Therapy Approvals 2017 (PDF). U.S. Food and Drug Administration (FDA) (Report). January 2018. Retrieved 16 September 2020.

[Rhopressa_FDA_label-1] "Rhopressa- netarsudil solution/ drops". DailyMed. Retrieved 2 May 2021.

[Rhokiinsa_EPAR-2] "Rhokiinsa EPAR". European Medicines Agency (EMA). 16 September 2019. Retrieved 27 September 2020.

[Dasso_2018-3] Dasso L, Al-Khaled T, Sonty S, Aref AA (2018). "Profile of netarsudil ophthalmic solution and its potential in the treatment of open-angle glaucoma: evidence to date". Clinical Ophthalmology. 12. Auckland, N.Z.: 1939–1944. doi:10.2147/OPTH.S154001. PMC 6177382. PMID 30323550.

[4] "Rhopressa (netarsudil) Ophthalmic Solution". U.S. Food and Drug Administration (FDA). 29 January 2018. Retrieved 3 June 2020.

[5] "Aerie (AERI) Gets Early FDA Approval for Lead Drug Rhopressa". 19 December 2017.

[6] New Drug Therapy Approvals 2017 (PDF). U.S. Food and Drug Administration (FDA) (Report). January 2018. Retrieved 16 September 2020.

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