On November 10, 2021 Lennham Pharmaceuticals, a privately-held company focused on the creative use of deuterium chemistry to improve the metabolic and pharmacological profile of existing compounds, reported the discovery and patenting of its next generation testosterone candidate, d3-testosterone (Press release, Lennham Pharmaceuticals, NOV 10, 2021, View Source [SID1234595144]).

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The U.S. Patent and Trademark Office (USPTO) has issued a Notice of Allowance for broad patent claims covering the use of d3-testosterone. Once issued, the patent will expire in 2041.

The allowed claims cover a method of treating male hypogonadism with d3-testosterone. Lennham’s patent disclosure covers numerous additional applications for d3-testosterone, including as a treatment for breast cancer, female sexual disorders, and as a gender affirming hormone therapy.

In non-clinical studies, d3-testosterone strongly resisted metabolism to the estrogen estradiol when compared to testosterone. Lennham’s non-clinical studies also demonstrated that d3-testosterone has similar androgen receptor agonist activity as testosterone. Lennham intends to present or publish data concerning d3-testosterone at upcoming scientific forums.

"Testosterone has demonstrated significant clinical benefit in treating a variety of conditions including breast cancer, female sexual dysfunction, male hypogonadism, and as gender affirming hormone therapy, but its therapeutic use has been limited in part because of estrogen-related side effects," said Bradford C. Sippy, Founder and CEO of Lennham. "Based on our preclinical studies and the scientific literature, we believe that d3-testosterone, by addressing estrogen-related limitations, has the potential to unlock the full therapeutic utility of testosterone therapy and become a best-in-class hormone treatment."

About Testosterone

Testosterone is a naturally occurring hormone that is found in both men and women. Products containing testosterone and prodrugs of testosterone, such as testosterone undecanoate, have been approved for use by FDA to treat certain conditions such as male hypogonadism and delayed puberty.

Testosterone is metabolized in humans to estradiol, 5α-dihydrotestosterone (DHT), and other hormones. The conversion of testosterone to estradiol, the primary estrogen metabolized from testosterone and the most prevalent estrogen in humans, is linked to several side effects of testosterone therapies, such as gynecomastia. It is reported that 30% of men using a testosterone therapy also use an aromatase inhibitor or and selective estrogen receptor modulator, products indicated to treat breast cancer, to reduce or treat symptoms of hyperestrogenism.1

Testosterone has been identified as a potentially useful treatment in other diseases and conditions, such as breast cancer2 and female sexual disorders3, but concerns about estradiol-related side effects such as breast cancer have limited its therapeutic potential4,5,6.

About Deuterated Testosterone

Deuterium is a naturally occurring, stable isotope of hydrogen, with an additional neutron in its nucleus. Selectively substituting hydrogen with deuterium, or deuteration, is a way to alter a molecule’s metabolic profile while maintaining its core pharmacodynamic characteristics.

Deuteration strengthens the chemical bond between two elements. Depending on where deuterium is placed, it has the potential to alter the overall metabolism of a molecule, or to reduce conversion to specific, unwanted metabolites.

Deuteration has been successfully leveraged in several approved and/or late-stage pharmaceutical products.

In non-clinical studies, d3-testosterone was shown to be highly resistant to metabolism to estradiol, potentially resulting in improved safety and tolerability profile versus testosterone.

Lennham’s allowed patent claims cover a method of treating hypogonadism in a male subject by orally, parenterally, or transdermally administering to the subject a pharmaceutical composition comprising between 1 mg and 1,000 mg of d3-testosterone, or a related prodrug.