Source: SyneuRx

Acting as Both a Dual Protease and TMPRSS2 Inhibitor, 

Pentarlandir® is About to Enter FDA Phase III Trial­

SyneuRx™ International, (Taipei Exchange, ticker ID TT6575, www.syneurx.com), a pioneering developer of novel CNS (Central Nervous System) and anti-viral pharmaceuticals, today announced that its investigational oral SARS-CoV-2 (COVID-19) anti-viral drug candidate Pentarlandir® has successfully demonstrated effectiveness against both the Omicron and Delta variants of the virus  in its preclinical studies. Pentarlandir® is currently in the final stage of a Phase II US-FDA trial (Phase III is scheduled to begin in 2022). 

Designed as an early-stage COVID-19 treatment, Pentarlandir® is given by mouth to patients suffering either from early-stage ‘breakthrough’ cases of COVID-19 (for those who have been previously vaccinated or infected) or potentially as a first-line treatment pathway for the unvaccinated who might otherwise face potential hospitalization and death. 

Pentarlandir® is indicated for the majority of COVID-19 patients – people who are in general good health with little risk of progressing to severe COVID-19 (that would result in hospitalization and death). In contrast, the Pfizer drug Paxlovid is designed for those who are at high risk of developing serious COVID-19 complications, (those aged 65 and older, or patients with comorbidities such as diabetes, obesity, heart or respiratory disorders). 

Given the natural origins of Pentarlandir®’s active chemical component, costs for the drug are expected to be significantly lower than for Paxlovid. As such, Pentarlandir® will be more accessible and affordable to less wealthy nations and as such represents an ideal solution to addressing the large worldwide population infected with the variant COVID-19 viruses.

How do Pentarlandir® and its competitor drugs stop COVID-19?

The Merck antiviral molnupiravir is considered a polymerase inhibitor, since it targets ribonucleic acid polymerase and inhibits COVID-19 as the RNA polymerase duplicates and introduces fatal errors into viral replication. The drug has a roughly 30% efficacy rate in preventing hospitalizations as demonstrated in early tests and as such is no longer considered a potential first-line treatment.

The Pfizer EUA drug Paxlovid combines two protease inhibitors for its viral attack vectors. Ritonavir is an existing drug used to combat HIV, while Nirmatrelvir is the brand name given to the experimental molecule PF-07321332, which was developed to specifically attack the protease of the COVID-19 virus. Protease is an integral enzyme within the virus that is necessary for proper replication. While Nirmatrelvir attacks the protease of COVID-19, ritonavir attacks the enzymes that would take on Nirmatrelvir, with both drugs operating in tandem to slow the replication of the virus.

Pentarlandir® is efficacious against COVID-19 and its variants by relying on a dual methodology to stop the virus – first acting as a protease inhibitor like Nirmatrelvir, but also acting as a TMPRSS2 inhibitor which acts to prevent the virus from infecting/entering cells in the first place. Unlike Paxlovid, Pentarlandir® is a single chemical with minimal documented side effects and is purified from natural sources, making it far less expensive to manufacture.

SyneuRx and Pentarlandir® Trials:

If successfully developed, SyneuRx intends to make Pentarlandir® available to the world’s developing nations as part of the United Nations-backed Medicines Patent Pool. More information about the Pentarlandir® Phase II trial can be found here: www.clinicaltrials.gov/ct2/show/NCT04911777

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