LPAR1 agonists(Lysophosphatidic acid receptor Edg-2 agonists), PLPPR2 agonists(phospholipid phosphatase related 2 agonists), PLPPR3 agonists(phospholipid phosphatase related 3 agonists)

Therapeutic Areas

Other DiseasesDigestive System Disorders

Active Indication-

Inactive Indication

Chemotherapy-induced nausea and vomitingDiarrheaRadiation Injuries+ [1]

Originator Organization

RxBio, Inc.

Active Organization-

Inactive Organization

RxBio, Inc.

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

100 Clinical Results associated with RX-100

100 Translational Medicine associated with RX-100

100 Patents (Medical) associated with RX-100

Literatures (Medical) associated with RX-100

01 Mar 2019·Journal of Lipid ResearchQ2 · BIOLOGY

Lysophosphatidic acid type 2 receptor agonists in targeted drug development offer broad therapeutic potential

Q2 · BIOLOGY

Review

Author: Lee, Sue Chin ; Szabo, Erzsebet ; Boler, Alyssa ; Norman, Derek D ; Thompson, Karin ; Balogh, Andrea ; Tigyi, Gabor J ; McCool, W Shannon ; Johnson, Leonard R

The growth factor-like lipid mediator, lysophosphatidic acid (LPA), is a potent signaling molecule that influences numerous physiologic and pathologic processes. Manipulation of LPA signaling is of growing pharmacotherapeutic interest, especially because LPA resembles compounds with drug-like features. The action of LPA is mediated through activation of multiple types of molecular targets, including six G protein-coupled receptors that are clear targets for drug development. However, the LPA signaling has been linked to pathological responses that include promotion of fibrosis, atherogenesis, tumorigenesis, and metastasis. Thus, a question arises: Can we harness, in an LPA-like drug, the many beneficial activities of this lipid without eliciting its dreadful actions? We developed octadecyl thiophosphate (OTP; subsequently licensed as Rx100), an LPA mimic with higher stability in vivo than LPA. This article highlights progress made toward developing analogs like OTP and exploring prosurvival and regenerative LPA signaling. We determined that LPA prevents cell death triggered by various cellular stresses, including genotoxic stressors, and rescues cells condemned to apoptosis. LPA₂ agonists provide a new treatment option for secretory diarrhea and reduce gastric erosion caused by nonsteroidal anti-inflammatory drugs. The potential uses of LPA₂ agonists like OTP and sulfamoyl benzoic acid-based radioprotectins must be further explored for therapeutic uses.

01 Sep 2018·Experimental Biology and MedicineQ4 · MEDICINE

Prevention and treatment of secretory diarrhea by the lysophosphatidic acid analog Rx100

Q4 · MEDICINE

Article

Author: Rao, Radakrishna ; Thompson, Karin E ; Ray, Ramesh M ; Shannon McCool, W ; Boler, Alyssa ; Ge, Wenbo ; Meena, Avtar S ; Alli, Shanta ; Tigyi, Gabor J ; Miller, Mark A ; Shukla, Pradeep K ; Johnson, Leonard R

Diarrheal disease is a severe global health problem. It is estimated that secretory diarrhea causes 2.5 million deaths annually among children under the age of five in the developing world. A critical barrier in treating diarrheal disease is lack of easy-to-use effective treatments. While antibiotics may shorten the length and severity of diarrhea, oral rehydration remains the primary approach in managing secretory diarrhea. Existing treatments mostly depend on reconstituting medicines with water that is often contaminated which can be an unresolved problem in the developing world. Standard treatments for secretory diarrhea also include drugs that decrease intestinal motility. This approach is less than ideal because in cases where infection is the cause, this can increase the incidence of bacterial translocation and the potential for sepsis. Our goal is to develop a safe, effective, easy-to-use, and inexpensive treatment to reduce fluid loss in secretory diarrhea. We have developed Rx100, which is a metabolically stable analog of lysophosphatidic acid. We tested the hypothesis that Rx100, similarly to lysophosphatidic acid, inhibits the activation of the cystic fibrosis transmembrane regulator Cl− channel and also reduces barrier permeability resulting in the decrease of fluid loss in multiple etiologies of secretory diarrhea. Here we have established the bioavailability and efficacy of Rx100 in cholera toxin-induced secretory diarrhea models. We have demonstrated the feasibility of Rx100 as an effective treatment for Citrobacter rodentium infection-induced secretory diarrhea. Using both the open- and closed-loop mouse models, we have optimized the dosing regimen and time line of delivery for Rx100 via oral and parenteral delivery.

100 Deals associated with RX-100

R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Diarrhea	Preclinical	US	RxBio, Inc.	23 Dec 2014
Stomach Ulcer	Preclinical	US	RxBio, Inc.	23 Dec 2014
Chemotherapy-induced nausea and vomiting	Preclinical	US	RxBio, Inc.	17 Jan 2007
Radiation Injuries	Preclinical	US	RxBio, Inc.	17 Jan 2007

Clinical Result

Indication

Phase

Evaluation

View All Results

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis


No Data

RX-100

Overview

Basic Info

Related

R&D Status

Clinical Result

Translational Medicine

Deal

Core Patent

Clinical Trial

Approval

Regulation