Tenpoint is Poised to Commercialize BRIMOCHOL, A Best-in-Class Therapy for Presbyopia

BRIMOCHOL delivers an unmatched combination of all-day duration and best-in-class tolerability achieved by the patented, synergistic combination of brimonidine and carbachol.

Tenpoint’s pipeline includes paradigm-shifting treatments for the largest ophthalmic indications with the greatest need and global market potential: presbyopia, cataracts and geographic atrophy.

Traditional ophthalmic drug development has resulted in therapeutics that only target one element of disease pathology, leading to pharmaceuticals with low responder rates and significant unmet needs. Tenpoint is transforming ophthalmic drug development by creating novel approaches and new chemical entities (NCEs) engineered to disrupt the multiple underlying disease pathologies inherent in sight-threatening diseases, presbyopia, cataract, and geographic atrophy. Our goal is to bring to market more comprehensive, disease-impacting therapeutics that preserve and restore vision, offering new hope for patients and the eye care professionals who treat them.

With our lead candidate BRIMOCHOL™ PF lighting the way and poised for commercialization, the therapeutics in our pipeline are engineered for efficacy and safety and offer great promise for patients who are experiencing or are at risk of vision loss.

Rejuvenating Vision for millions of presbyopes

BRIMOCHOL IS UNIQUE

BRIMOCHOL PF ^TM is a proprietary pupil-modulating eye drop that combines two well-studied, FDA-approved pharmaceuticals: carbachol (a cholinergic agent) and brimonidine tartrate (an alpha-2 agonist).
Together, they produce a “pinhole effect,” which reduces the size of the pupil so that only centrally focused light rays are able to enter the eye, thereby sharpening distant and near images while minimizing side effects.
The result is clarity of vision for near tasks like reading or using a smartphone.
This patented combination eye drop has been studied in more than 600 patients, 45-80 years of age, across 47 sites in the United States.
The first of two pivotal Phase 3 trials (BRIO-I and BRIO-II) are complete, with topline date for BRIO-II expected in 2H, 2024.

BRIMOCHOL MECHANISM OF ACTION

Carbachol is the most potent and durable miotic agent for pupil constriction,¹ while brimonidine tartrate is a sympatholytic alpha-2 agonist that prevents pupil dilation. Miotics reduce the size of the pupil, creating a “pinhole” effect that results in an improvement in near visual acuity.
The addition of brimonidine tartrate, an inhibitor of iris dilator muscle contraction, may also inhibit the contraction of the ciliary muscle by activating alpha-2 receptors, potentially mitigating the side effects commonly associated with miotics.²
Brimonidine tartrate also appears to increase the bioavailability of carbachol by altering aqueous dynamics, prolonging the pinhole effect^3,4 and contributing to a longer duration of action.⁵

WHAT IS PRESBYOPIA?

Presbyopia is a natural, inevitable part of the aging process and the most common cause of vision impairment. Loss of near vision typically begins when adults reach their mid-40s, and the condition is almost universal by age 50.⁶ The vast majority of people will experience presbyopia in their lifetime. It is estimated that presbyopia will affect 2.1 billion people globally in 2020, with approximately 128 million residing in the US.^7,8

CAUSES OF PRESBYOPIA

The clear lens in the eye focuses light onto the retina. In younger people, the lens is soft and flexible and changes shape easily, which is what allows us to shift focus between near and distant objects.
As we age, the lens becomes more rigid and isn’t able to change shape as easily, making it more difficult to focus up close.

MEET THE SCIENTIST WHO DISCOVERED BRIMOCHOL™

Tenpoint Therapeutics’ lead product candidate, BRIMOCHOL PF, was developed by Dr. Herb Kaufman, a renowned researcher and inventor in ophthalmology. He is perhaps best known for discovering and developing the world’s first antiviral drug for the treatment of virus infection, which led to the introduction of the combination of steroid and antiviral therapy for stromal keratitis in 1962. This achievement was followed by more than 15 research discoveries over his lifetime, which significantly advanced patient care in ophthalmology and beyond. After retiring in 2008 from his role as Emeritus Boyd Professor of Ophthalmology and Pharmacology & Experimental Therapeutics at LSU, instead of basking in retirement life, Dr. Kaufman, along with one of his former fellows, quietly led a research initiative that would eventually culminate in the development of BRIMOCHOL PF.

1. Stamper RL, Lieberman MF, Drake MV, eds. Becker-Shaffer's Diagnostics and Therapy of the Glaucomas. 8th ed. Mosby; 2009.
2. Kubo C, Suzuki R. Involvement of prejunctional alpha 2-adrenoceptor in bovine ciliary muscle movement. J Ocul Pharmacol. 1992;8(3):225-231. doi:10.1089/jop.1992.8.225
3. Data on File
4. Data on File
5. Abdelkader A. Influence of Different Concentrations of Carbachol Drops on the Outcome of Presbyopia Treatment—A Randomized study. International Journal of Ophthalmic Research. 2019;5(1):317-319.
6. Mancil GL, Bailey IL, Brookman KE, et al; American Optometric Association Original Consensus Panel on Care of the Patient with Presbyopia. Optometric Clinical Practice Guideline: Care of the Patient With Presbyopia. American Optometric Association; 2011.
7. Zebardast et al. The Prevalence andDemographic Associations of Presenting Near-Vision Impairment Among AdultsLiving in the United States. Am J Ophthalmol. 2017;174:134-144.8. U.S. Census Bureau. Table 9. Washington: Population Division. 2014.

A NOVEL COMBINATION EYE DROP