MIPS Project Detail:

Firefox Pharmaceuticals, LLC

Enhancers of Reverse Cholesterol Transport

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Company

Firefox Pharmaceuticals, LLC

Baltimore

Baltimore City

County

, Maryland

Founded:

2017

Website:

Company Description:

Firefox Pharmaceuticals is a start-up biotechnology company developing and commercializing a novel class of cholesterol-lowering drugs, creating first-in-class small molecules for reverse cholesterol transport enhancers (RCTE). After nine years of uninterrupted academic research and pharmaceutical R&D, the company has made discoveries in the direct reverse cholesterol transport (RCT) process. Firefox’s strategy tackles all four RCT steps: 1.) increase nascent HDL availabilities; 2.) increase macrophage cholesterol efflux; 3.) increase cholesterol esterification; and 4) increase liver uptake for fecal excretion. Others have focused on strategies to increase HDL (and decrease LDL). Firefox’s quadruple-pronged plan of attack could reduce cholesterol to unprecedented levels by enhancing RCT and eliminating cholesterol already present. The company’s lead compound has showed desired activities, both in vitro and in vivo, for enhanced RCT. A patent application was filed with USPTO on April 3, 2017.

MIPS Project

Enhancers of Reverse Cholesterol Transport

Project #

6011.24

|

MIPS Round

64 |

Starting Date:

Aug 2019

MIPS Project Challenge:
The goal of this MIPS project is to design and synthesize a series of analogs for Firefox’s lead compound, FFP-001, that could be drug candidates. The company will perform both in vitro and in vivo biological evaluations of these compounds, which will lead to the selection of optimized candidate compounds.

Project Scope:
Researchers in this MIPS project will design and synthesize a series of analogs to the company’s lead compound, FFP-001, which would improve FFP-001’s invitro and in-vivo activities for facilitating cholesterol efflux and reducing cellular cholesterol mass, and directly enhancing RCT. The company will then test these compounds using a number of in-vivo mice and rabbit models. Data compiled from these studies will be used in an iterative process to inform subsequent rounds of analog design and synthesis, thereby improving the activities of subsequent analogs. The company anticipates that the laboratory will produce 60-100 new analogs within 12 months, with 1-3 drug candidate compounds being compared in pre-clinical studies in year two. Also in year two, researchers plan to scale up the synthesis of the selected 1-3 candidate compounds (in grams) from Phase 1 of the project, producing sufficient quantifies for pre-clinical studies.

There are three major mechanisms for lowering cholesterol; two of them have generated blockbuster drugs: 1.) inhibit de novo cholesterol production (synthesis), Lipitor (statins); 2.) reduce dietary cholesterol absorption, Zetia/Ezetimibe; and 3.) Reverse Cholesterol Transport enhancers (RCTE), the “Holy Grail” in lowering cholesterol, for which no drugs have been developed, in this large, unmet market.

Source: Firefox Pharmaceuticals

Results:

Approximately 73.5 million adults (31.7 percent) in the U.S. have high cholesterol, which is one of the major causes of heart disease, the leading cause of death. Every year, 610,000 American die from heart disease. The annual cholesterol-lowering drug market is more than $20 billion.

Source: Firefox Pharmaceuticals