REL-1015 (LevoCap ER)

A novel version of a proven drug product, REL-1015 (LevoCap ER), is an extended release, abuse deterrent, proprietary formulation of the opioid analgesic levorphanol, which is pharmacologically differentiated from morphine, oxycodone, and other strong opioids for the management of pain severe enough to require daily, around-the-clock, long-term opioid treatment. In particular, levorphanol binds to all three opioid receptor subtypes involved in analgesia (mu, kappa, and delta), the N-methyl-D-aspartate (NMDA) receptor and the norepinephrine and serotonin uptake pumps, whereas morphine is relatively selective for mu sites. The dual mechanism of action of levorphanol, combining opioid receptor agonism with noradrenaline reuptake inhibition in the same molecule makes levorphanol a useful analgesic to treat chronic and neuropathic pain in addition to providing pain relief in patients resistant to other strong opioids. Levorphanol is a strong opioid first developed in the 1940s as an alternative to morphine and has greater potency than morphine. In clinical studies, it has demonstrated a remarkably broad spectrum of analgesic activity against many different types of pain including neuropathic pain, post-surgical pain, and chronic pain in patients refractory to other opioids.

REL-1015 (LevoCap) has completed Phase 1 studies. Under the 505(b)2 regulatory pathway, LevoCap could go directly into Phase 3 studies. There are no current studies ongoing.

Key Points

  • Clinically and pharmacologically differentiated from other strong opioids 

  • Effective in nociceptive and neuropathic pain
  • Once or twice a day extended release formulation 

  • Abuse deterrent and tamper resistant

Market Potential

The chronic pain market is a very large market with growth expected in certain segments including cancer pain, low back pain and osteoarthritis in line with the aging population. In the US alone, there were 334 million prescriptions written for pain in 2014. In financial terms the market is valued at $21 billion globally with approximately $14 billion in the US. Relmada expects that REL-1015 will be positioned for patients who require an opioid for moderate to severe chronic pain with a neuropathic component or mixed neuropathic/nociceptive pain (cancer patients, low back pain).

Potential Large Target Populations

  • Cancer pain
  • Chronic non-cancer pain
    • Osteoarthritis
    • Low back pain
    • Idiopathic pain
  • Neuropathic pain

How it Works

REL-1015's multi-modal mechanism of action provides for a more robust efficacy profile and could potentially be used alone for patients who take multiple drugs.

Opioid Mechanism
Ascending Pathways

Works to inhibit pain by binding to opioid receptors.

how it works

Non-Opioid Mechanism
Descending Pathways

Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs) affect the nerve cells in the brain and inhibit the reuse of specific neurotransmitters to enhance inhibition of pain signaling.