Antibe to have Phase 2 pain data by third quarter

Dan Legault, CEO

Dan Legault, CEO

Antibe Therapeutics (OTCQB:ATBPF; TSX-V:ATE) expects to have data by the third quarter this year from a small Phase 2 study of its naproxen derivative, ATB-346, in patients with osteoarthritis in the knee.

“ATB-346 was designed to deliver non-addictive pain relief with significantly less gastrointestinal and cardiovascular damage than is typically associated with the use of non-steroidal anti-inflammatory drugs (NSAIDs),” CEO, Dan Legault, says in an interview with BioTuesdays.com.

NSAIDs are among the most widely used drugs in the world and represent a $12-billion global market. They include prescription and over-the-counter brands such as naproxen (Aleve), celecoxib (Celebrex), ibuprofen (Advil) and Aspirin. However, GI damage with NSAIDs is pervasive and a safer treatment of pain and inflammation could be a blockbuster game changer.

In addition to a portfolio of pain and inflammation candidates, Antibe, which takes its name from Claude Monet paintings of the town, Cap d’Antibes on the French Riviera, is pursuing both product and business development opportunities to support growth of its regenerative medicine portfolio, targeting tissue regeneration in oral and maxillofacial surgery.

Mr. Legault explains that ATB-346 is a hydrogen sulfide-releasing derivative of naproxen, which is among the most commonly used and most cardiovascular-safe of the NSAID class.

“Our patent-protected drug development technology enables the linking of an NSAID molecule to a hydrogen sulfide-releasing molecule,” he adds.

Hydrogen sulfide is utilized throughout the body, serving as an anti-inflammatory agent and signaling molecule. Combined with an expanding scope of indications for NSAID use, Mr. Legault points out that the unique properties of hydrogen sulfide have the potential to substantially improve medicines for pain and inflammation across the spectrum of human illness.

In preclinical studies, ATB-346 produced negligible GI damage over the full range of human dosing, unlike comparator NSAIDs, he contends. In addition, in conditions of increased susceptibility to gastric damage, the GI damage from comparator NSAIDs increased significantly, while ATB-346 remained GI safe.

ATB-346 was designed to deliver non-addictive pain relief with significantly less gastrointestinal and cardiovascular damage than is typically associated with the use of non-steroidal anti-inflammatory drugs

ATB-346 was designed to deliver non-addictive pain relief with significantly less gastrointestinal and cardiovascular damage than is typically associated with the use of non-steroidal anti-inflammatory drugs

“Extensive scientific work after a Phase 1 trial strongly suggested that a lower dose of ATB-346 is much more potent and long lasting than had been predicted from animal studies,” he adds.

The primary endpoint of the Phase 2 trial is clinical assessments of pain and inflammation over the course of 10 days of treatment with ATB-346 at 250mg once daily, which is several times less than the dose used in the Phase 1 study.

“We’ll analyze the data after the current trial and then decide on performing dose-ranging and proof-of-concept Phase 2 studies,” Mr. Legault says.

Antibe’s next pain candidate is ATB-352, which Mr. Legault says causes negligible intestinal damage in rats, compared with ketoprofen, an NSAID prescribed for acute pain. Ketoprofen is a powerful NSAID but doctors do not prescribe it for more than a few days because of its potential for GI damage.

“We won’t start the IND-enabling preclinical studies with ATB-352 until we have further data from ATB-346,” he adds.

Mr. Legault says Antibe also has done rat studies with its Aspirin-derivative, ATB-340, and found that it does not contribute to bleeding ulcers the way Aspirin does. Small doses of Aspirin, however, can provide cardiovascular benefits and a recent major study has linked Aspirin to prevention of digestive system cancers.

In regenerative medicine, Antibe is focused on oral health as a global growth strategy. “We see lots of opportunity to internally develop and in-license the highest value products that address dental regenerative medicine,” he suggests.

ATB-346 produced negligible GI damage over the full range of human dosing, unlike comparator NSAIDs

ATB-346 produced negligible GI damage over the full range of human dosing, unlike comparator NSAIDs

Antibe’s wholly-owned subsidiary, Citagenix, sells a portfolio of tissue regenerating products to the dental and orthopedic markets. Since its inception in 1997, Citagenix has become the largest source of knowledge and experience in the Canadian medical device industry, Mr. Legault suggests.

Citagenix is active in 15 countries, operating in Canada through a direct sales force of 10 people, and internationally via a network of distributors. “Our next big focus will be expanding our distribution footprint in the U.S.,” he adds.

Citagenix’s products include bone-grafting solutions, such as scaffolds and demineralized bone matrix products that display both osteoconductive and osteoinductive activity; and allogeneic and xenogeneic soft-tissue grafts that support guided tissue regeneration and guided bone regeneration.

In April, Citagenix launched PentOS OI Putty, the first product of a new family of bone graft substitutes that have a proven ability to form bone. PentOS OI Putty is a demineralized bone matrix made from 100% human bone and does not contain any extrinsic carriers. Three additional PentOS OI products are expected to launch in the coming months, including PentOS OI Flex, PentOS OI Sponge and PentOS OI Fill.

Antibe’s wholly-owned subsidiary, BMT Medizintechnik of Germany, designs, manufactures and markets a complete product portfolio of over 10,000 surgical instruments, with major distributors located throughout Europe, the Americas, the Middle East and Asia.

Antibe’s lead pain candidate also may play a role in regenerative medicine.

Mr. Legault says the company has published results of a study that demonstrated Antibe’s hydrogen sulfide-release naproxen derivative, ATB-346, inhibits alveolar bone loss and inflammation in rats with periodontitis, or inflammation of the gums, suggesting it may be a valuable adjuvant therapy for periodontal disease.

NSAIDs, such as naproxen (Aleve), have known adverse effects on bone growth.

“Doctors are increasingly appreciating the impact of oral health on overall health,” he says, noting that bacteria impacting dental decay are a major colonizer of arterial plaque in diseased heart patients. In addition, periodontal disease has a strong connection to inflammation and diabetes.

Antibe's Clinical Development Pipeline

Antibe's Clinical Development Pipeline