Delving into the Latest Updates on MOL-6131 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

Tryptase

Mechanism

Tryptase inhibitors

Therapeutic Areas

Immune System DiseasesRespiratory Diseases

Active Indication-

Inactive Indication

Asthma

Originator Organization

Molecumetics Ltd.

Active Organization-

Inactive Organization

JW PHARMACEUTICAL Corp.Molecumetics Ltd.

Drug Highest PhaseDiscontinuedDiscovery

First Approval Date-

Regulation-

AbstractRelease of human lung mast cell tryptase may be important in the pathophysiology of asthma. We examined the effect of the reversible, nonelectrophilic tryptase inhibitor MOL 6131 on airway inflammation and hyper-reactivity in a murine model of asthma. MOL 6131 is a potent selective nonpeptide inhibitor of human lung mast cell tryptase based upon a β-strand template (Ki = 45 nM) that does not inhibit trypsin (Ki = 1,061 nM), thrombin (Ki = 23, 640 nM), or other serine proteases. BALB/c mice after i.p. OVA sensitization (day 0) were challenged intratracheally with OVA on days 8, 15, 18, and 21. MOL 6131, administered days 18–21, blocked the airway inflammatory response to OVA assessed 24 h after the last OVA challenge on day 22; intranasal delivery (10 mg/kg) had a greater anti-inflammatory effect than oral delivery (10 or 25 mg/kg) of MOL 6131. MOL 6131 reduced total cells and eosinophils in bronchoalveolar lavage fluid, airway tissue eosinophilia, goblet cell hyperplasia, mucus secretion, and peribronchial edema and also inhibited the release of IL-4 and IL-13 in bronchoalveolar lavage fluid. However, tryptase inhibition did not alter airway hyper-reactivity to methacholine in vivo. These results support tryptase as a therapeutic target in asthma and indicate that selective tryptase inhibitors can reduce allergic airway inflammation.

100 Deals associated with MOL-6131

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Asthma	Discovery	US	JW PHARMACEUTICAL Corp.	-
Asthma	Discovery	US	Molecumetics Ltd.	-
Asthma	Discovery	US	JW PHARMACEUTICAL Corp.	-
Asthma	Discovery	US	Molecumetics Ltd.	-