Our second-most-advanced novel version of a proven drug product, REL-1028 (BuTab), represents novel oral formulations of modified release buprenorphine being developed for both chronic pain and opioid dependence indications. Buprenorphine is a partial opioid agonist that has been widely used by the sublingual and transdermal routes of administration, but was believed to be ineffective by the oral route due to low bioavailability. REL-1028 is a proprietary formulation of buprenorphine that is designed to overcome the significant first pass metabolism in the upper gastrointestinal tract to allow for oral administration in traditional capsule or tablet form. We have completed a preclinical program to better define the pharmacokinetic profile of REL-1028 and to assess the time course of systemic absorption of buprenorphine using several different oral modified release formulations of buprenorphine in dogs, compared to an intravenous administration.
|Preclinical||Phase 1||Phase 2||Phase 3|
Projected stage of development in 12-24 months
- Potentially the first traditional tablet form of buprenorphine designed to deliver safe and effective blood levels through the gastrointestinal route of administration
- In development for both addiction and management of moderate to severe chronic pain
- Schedule-III opioid; reduced risk of drug abuse and physical dependence
- Being developed under the 505(b)(2) regulatory pathway
- Can go directly into Phase III (no Phase II study required)
By the Numbers
U.S. individuals addicted to opioids
Percentage of U.S. physicians who write 90% of buprenorphine prescriptions; easy access to physicians through a small and concentrated prescriber base
Market Potential for Pain Treatment
The pain market is well established, with many pharmaceutical companies marketing innovative products as well as generic versions of older, non-patent protected products. In 2014, according to data from IMS Health, there were 328 million pain prescriptions representing $13 billion in annual sales in the U.S.
Market Potential for the Treatment of Addiction
Maintenance treatment with buprenorphine reduces the typical cravings and withdrawal symptoms associated with coming off opioid prescription painkillers and heroin. This allows the individual suffering from an addiction to opioids –along with counseling and support – to work toward recovery. On average, treatment lasts a couple months, reflecting relatively high dropout rates, but a significant number of people remain on buprenorphine treatment chronically, with nearly one-quarter of patients still on therapy after nine months.
The total market for buprenorphine containing products for opioid dependence approached $1.8 billion in 2014. The market has grown significantly as a result of the rapidly escalating problem of prescription opioid misuse and abuse, a recent resurgence of heroin use, the growing number of physicians treating opioid dependence, and the inclusion of addiction treatment as an essential benefit in the Affordable Care Act.
Enrollment in Relmada Therapeutics' Proof-of-Concept Clinical Study for Novel Oral Formulations of Buprenorphine Reaches Halfway Mark
Relmada Therapeutics announces patient enrollment in its proof-of-concept pharmacokinetic study with novel formulations of oral, enteric-coated buprenorphine (collectively BuTab, or REL-1028) being developed for both chronic pain and opioid dependence indications has reached the halfway point. Consistent with prior guidance, the company anticipates reporting top-line results in the second half of 2015.