OxyNal (oxycodone/naltrexone) / Elite Pharma, Acura Pharma - LARVOL DELTA

Genome and transcriptome of Papaver somniferum Chinese landrace CHM indicates that massive genome expansion contributes to high benzylisoquinoline alkaloid biosynthesis. (PubMed, Hortic Res) - "Opium poppy (Papaver somniferum) is a source of morphine, codeine, and semisynthetic derivatives, including oxycodone and naltrexone...Variations between the 2.62 Gb CHM genome and that of the previously sequenced high noscapine 1 (HN1) variety were also explored...Genes carrying structural variations and large-effect variants associated with agronomically different phenotypes between CHM and HN1 that were identified through our transcriptomic comparison of multiple organs and developmental stages can enable the development of new varieties. These genomic and transcriptomic analyses will provide a valuable resource that informs future basic and agricultural studies of the opium poppy."

Journal

Methylnaltrexone crosses the blood-brain barrier and attenuates centrally-mediated behavioral effects of morphine and oxycodone in mice. (PubMed, Neuropharmacology) - "These results provide converging behavioral and analytical evidence that MNTX administration in mice attenuates centrally-mediated effects produced by opioid analgesics and results in functional concentrations of MNTX and NTX in blood and brain. Collectively, these findings indicate that MNTX cannot be administered systemically in mice for making inferences that its effects are peripherally restricted."

Journal • Addiction (Opioid and Alcohol) • Pain

Stereoselective syntheses of 3-dehydroxynaltrexamines and N-methyl-3-dehydroxynaltrexamines. (PubMed, Tetrahedron Lett) - "A stereoselective route is provided for each target compound while a novel one-pot method for the synthesis of 6 α/β-3-N-methyl-3-dehydroxynaltrexamines is also explored. These results enable the versatile and efficient preparation of key epoxymorphinan intermediates to facilitate future selective opioid ligand discovery and development."

Journal

SAD: Study of PF614 Compared to OxyContin® in Healthy Volunteers (clinicaltrials.gov) - P1; N=64; Recruiting; Sponsor: Ensysce Biosciences; Completed ➔ Recruiting; N=48 ➔ 64; Trial primary completion date: Apr 2017 ➔ Jan 2018

Enrollment change • Enrollment open • Trial primary completion date • Biosimilar

Emerging therapies for patients with symptoms of opioid-induced bowel dysfunction. (PubMed) - "Thus, a complex assessment and management that addresses underlying causes and patomechanisms of OIBD is recommended. Newer strategies comprise methylnaltrexone or OXN administration in the management of OIBD, and OXN may be also considered as a preventive measure of OIBD development in patients who require opioid administration."

Review • Biosimilar • Oncology • Pain