REL-1028 (BuTab)

A 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.

REL-1028 (BuTab) has completed a single dose PK study in 18 patients. Under the 505(b)2 regulatory pathway, LevoCap does not need to complete Phase 2 studies and could potentially go directly into Phase 3 studies. There are no current studies ongoing.

Key Points

  • 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

By the Numbers

2 Million

U.S. individuals addicted to opioids

<1%

Percentage of U.S. physicians who write 90% of buprenorphine prescriptions; easy access to physicians through a small and concentrated prescriber base