Delving into the Latest Updates on H-1337 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

LRRK2 x PKA x PKD1 x PKN2

Action

inhibitors

Mechanism

LRRK2 inhibitors(Leucine-rich repeat serine/threonine-protein kinase 2 inhibitors), PKD1 inhibitors(polycystin 1, transient receptor potential channel interacting inhibitors), PKN2 inhibitors(protein kinase N2 inhibitors)

+ [1]

Therapeutic Areas

Eye Diseases

Active Indication

Glaucoma 1, Open Angle, A

Inactive Indication-

Originator Organization

D. Western Therapeutics Institute, Inc.

Active Organization

D. Western Therapeutics Institute, Inc.

Inactive Organization

Allysta Pharmaceuticals, Inc.

License Organization-

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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PURPOSETo perform a phase Ⅰ/Ⅱ evaluation of an H-1337 ophthalmic solution in subjects with primary open-angle glaucoma (POAG) or ocular hypertension (OHT).DESIGNThis was a phase I/II, randomized, double-masked, vehicle-controlled, dose-response study conducted at 6 private practice sites in the United States. The study was registered with clinicaltrials.gov as NCT03452033.PARTICIPANTSEighty-seven subjects with bilateral POAG or OHT were enrolled.METHODSAfter washout of ocular hypotensive medications as required, the subjects were randomized to receive either the H-1337 ophthalmic solution at 0.06%, 0.2%, and 0.6% or its vehicle twice daily unilaterally in the study eye for the first 3 days and then twice daily in both eyes from day 4 to 28.MAIN OUTCOME MEASURESThe primary efficacy end point was the mean change in intraocular pressure from baseline (day 0) for each group on day 28 at hour 4 compared with the vehicle.RESULTSIn the primary efficacy end point, i.e., mean change from the baseline on day 28 at hour 4, the mean change from the baseline was - 4.45 ± 3.801, - 5.16 ± 3.114, - 4.93 ± 3.110, and - 0.39 ± 2.355 in the 0.06%, 0.2%, and 0.6% H-1337 and vehicle groups, respectively. The difference between each active group and the vehicle group was statistically significant (P < 0.0001). Treatment-emergent adverse events (TEAEs) occurred in 49% of subjects who received H-1337 (range, 41% [0.2% arm]-64% [0.6% arm] across the H-1337 arms) and 18% of subjects who received the vehicle. The majority of TEAEs were mild in severity; 3 subjects who received H-1337 had a TEAE of moderate intensity (instillation site erythema, blurred vision, and muscle strain).CONCLUSIONSThe H-1337 ophthalmic solution showed clinically and statistically significant ocular hypotensive activity and was well tolerated, with a relatively low incidence of hyperemia.FINANCIAL DISCLOSURE(S)Proprietary or commercial disclosure may be found after the references.

01 Jan 2008·Molekuliarnaia genetika, mikrobiologiia i virusologiia

[Difference in amino acid sequences of B. afzelii P66 surface-exposed loop region].

Article

Author: Korenberg, E I ; Morozov, A V ; Gorelova, N B ; Fadeeva, I A

In the present work, we performed a phenotyping analysis of 45 B. afzelii 89-a.a. long amino acid sequences of 7 different allele variants, corresponding to the surface-exposed loop region of P66. 45 investigated isolates showed 5 phenotypically different variants; 2 phenotypically different variants of loop region, in particular, also showed mutations in the putative monoclonal antibody H1337 binding site; the similarity between the amino acid sequences taken from different variants is about 96.66% to 98.88%; in one natural locus up to 3 different phenotypes of P66 could circulate simultaneously.

Investigative Ophthalmology & Visual Science

Elucidation of molecular mechanism of H-1337, an anti-glaucoma agent

Author: Kei Hasegawa ; Yoko Yoshida ; Atsuko Kasai ; Hiroyoshi Hidaka

100 Deals associated with H-1337

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Glaucoma 1, Open Angle, A	Phase 2	United States	D. Western Therapeutics Institute, Inc.	28 Aug 2023
Glaucoma, Open-Angle	Preclinical	United States	Allysta Pharmaceuticals, Inc.	15 Mar 2018

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03452033 (CTgov)	Phase 1/2	Glaucoma, Open-Angle	87	H-1337 (H-1337 0.06%)	(cfmxnqftoy) = endnskcjsc kxunxjttsv (mwuzeewrya, lsvczpaxju - bevteqccxj) View more	-	02 Aug 2021
				H-1337 (H-1337 0.2%)	(cfmxnqftoy) = eovtkoaffv kxunxjttsv (mwuzeewrya, jgyzkfuhsv - qerndpwdur) View more
ARVO2015	Not Applicable	Wet age-related macular degeneration	-	H-1337	(lnpepgcqfa) = ycjovwsjmc fcslnsuftx (komkbwohir ) View more	-	01 Jun 2015
				H-1337M1	(lnpepgcqfa) = ksaewhwdej fcslnsuftx (komkbwohir ) View more
ARVO2015	Not Applicable	Ocular Hypotension	-	H-1337	(hmhxdehzqh) = glnzzggkey ixkrrjlrut (myknievvey )	-	01 Jun 2015