PF05 Reduce Opioid-Associated Side Effects

Market

In the U.S. alone, opioid prescriptions exceed 200 million annually. Up to 90% of patients taking opioids experience opioid-associated side effects, including opioid-induced constipation (OIC).

Unmet Need

The pain relief provided by opioid drugs Medications made from, artificially developed from, or containing opium, a potent pain-killing substance that is derived from poppy pods. Examples of opioid medications include morphine, codeine and hydrocodone. results from their interaction with µ-opioid receptors in the central nervous system. However, opioid drugs also interact with µ-opioid receptors outside of the central nervous system (i.e., in the periphery), and these interactions result in many debilitating side effects – such as, constipation, bladder dysfunction, itching, and nausea.

Although often dismissed as a trivial side effect, constipation adversely affects a patient’s quality of life. Severe constipation can force patients to reduce their opioid dose, resulting in inadequate pain relief. Furthermore, chronic constipation can result in rectal pain and burning, bowel obstruction, bowel perforation, and death.

Currently, there is no oral, peripherally-restricted opioid antagonist approved for the treatment of opioid-induced constipation.

PharmacoFore's Solution

The objective of our PF05 program is an oral treatment to reduce opioid-associated side effects. PF05 acts as an antagonist on the peripherally located µ-opioid receptors in associated with the gastrointestinal (GI) tract, and is designed to alleviate the OIC.

A PF05 product candidate could either be taken alone or co-formulated with our Bio-Activated Molecular Delivery™ abuse-resistant opioids. Combining these innovative discoveries will improve patients’ quality of life, reduce morbidity and mortality by providing effective pain relief with reduced side effects, while lowering the risks of misuse and abuse.

We have discovered orally bioavailable, highly potent (activity similar to naltrexone), peripherally restricted µ-opioid antagonists. In pre-clinical studies, lead candidates have demonstrated oral efficacy in reversing opioid-agonist-induced effects on GI transit times.