- Human PK study shows that d9-caffeine produced a similar time to peak, a ~30% higher peak exposure, and a ~4-fold higher overall exposure than a similar dose of caffeine
- Animal and in vitro studies demonstrate that d9-caffeine is non-mutagenic and exhibits similar adenosine receptor activity to normal caffeine
- d9-Caffeine is potentially a safe, well-tolerated, and long-lasting alternative to caffeine
CONCORD, Mass.–(BUSINESS WIRE)–Lennham Consumer Products, a start-up focused on the creative use of deuterium chemistry to improve well-known products, today announced the publication of two manuscripts describing the clinical and non-clinical pharmacokinetics (PK) and safety of d9-caffeine.
The first manuscript, published in Regulatory Toxicology and Pharmacology, reports the results of the first-ever human PK study comparing d9-caffeine to a similar dose of normal caffeine at two dose levels. The study demonstrated that d9-caffeine produced a similar time to peak, a ~30% higher peak exposure, and a ~4-fold higher overall exposure than normal caffeine. d9-Caffeine also demonstrated a 5-10-fold lower relative exposure to the primary metabolites of caffeine. Results indicate that both d9-caffeine and normal caffeine were well tolerated, and no adverse events for insomnia were reported. The full manuscript can be read here.
The second manuscript, published in Food and Chemical Toxicology, reports on studies examining the non-clinical safety, pharmacology, and pharmacokinetics of d9-caffeine. The studies demonstrate that d9-caffeine has similar adenosine receptor activity to caffeine, is non-mutagenic, and crosses the blood-brain barrier in mammals. The full manuscript can be read here.
“In 2019, Lennham set out to improve caffeine by creating an enhanced version that provides the same benefits but lasts longer. Our peer-reviewed publications demonstrate that we have achieved that goal,” said Bradford C. Sippy, Founder of Lennham. “Lennham believes that d9-caffeine has the potential to be a unique, highly differentiated product that could be used in multiple applications, including as a substitute for normal caffeine in energy drinks. The publication of these manuscripts is a critical step in Lennham’s pursuit of a general recognized as safe (GRAS) designation for use of d9-caffeine as a food and beverage ingredient.”
Caffeine is the most widely consumed psychoactive agent in the world. While caffeine is a safe1,2 and effective stimulant, it is quickly cleared by the body following a rapid onset, even at high doses, causing what is known colloquially as the “caffeine crash”. Caffeine is primarily metabolized by the CYP450 isoenzyme CYP1A2. Genetic polymorphs of CYP1A2 exist that may influence the metabolism of caffeine.3
d9-Caffeine is a longer-lasting version of caffeine that is enriched with deuterium. Unlike extended-release caffeine products, which have failed to achieve the Tmax and Cmax of caffeine, d9-caffeine has demonstrated substantially differentiated pharmacokinetics, including a similar Tmax, higher Cmax, longer half-life, and reduced relative exposure to the primary metabolites of caffeine. d9-Caffeine has been shown to be similarly metabolized in slow vs. fast metabolizers of caffeine.
Deuterium is a naturally occurring, stable, non-toxic isotope of hydrogen, with an additional neutron in its nucleus. Selectively substituting protium (the most prevalent form of hydrogen) with deuterium, or deuteration, is a way to alter a molecule’s metabolic profile while maintaining the 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.
About Lennham Consumer Products
Lennham Consumer Products is a Division of Lennham Pharmaceuticals. Lennham is a privately held, clinical-stage life sciences company focused on the creative application of deuterium chemistry to improve upon highly utilized and well-characterized compounds. Founded in 2019, Lennham’s unique approach to deuteration has enabled it to rapidly develop a pipeline of product candidates, including deuterium-enriched forms of caffeine, testosterone, and psilocybin.
For more information, please visit www.lennham.com.
- van Dam RM et al. Coffee, Caffeine, and Health. N Engl J Med. 2020 Jul 23;383(4):369-378.
- FDA Code of Federal Regulations. 21CFR182.1180. Accessed 03 Jun 2021.
- Nehlig A. Interindividual Differences in Caffeine Metabolism and Factors Driving Caffeine Consumption. Pharmacological Reviews. 2018, 70:384-411.
Chief Business Officer
Lennham Consumer Products