PTX-008 (OTX008) is a calixarene-based compound and galectin-1 (Gal-1) inhibitor with potential anti-angiogenic and antineoplastic activities. Upon subcutaneous administration, galectin-1 inhibitor OTX008 binds Gal-1 which leads to Gal-1 oxidation and proteosomal degradation through a not yet fully elucidated mechanism, and eventually downregulates Gal-1. This decreases tumor cell growth and inhibits angiogenesis. Gal-1, a multifunctional carbohydrate-binding protein, is often overexpressed on tumor cells and plays a key role in cancer cell proliferation, apoptosis, tumor angiogenesis and evasion of immune responses. PTX-008 had been in phase I clinical trials for the treatment of solid tumours. This compound was originally discovered by University of Minnesota and PepTx, then licensed to OncoEthix (acquired by Merck Sharp & Dohme in 2014). However, no recent developments has been reported.

Cannabidivarin is a homolog of cannabidiol, with a well-established antiepileptiform profile in preclinical studies, both in vitro and in vivo animal models of epilepsy. The oral bioavailability of cannabidivarin is very low (about 6%) due to erratic absorption and first pass metabolism. After oral administration, the maximum plasma concentration of Cannabidivarin is rising in about three hours and the drug has a large volume of distribution, because of his link to protein plasma, being highly liposoluble, so CBDV can penetrate well to the brain. Cannabidivarin is also metabolized in the liver to 7-COOH and 6-OH metabolites, but the mechanism is also unknown. There is an ongoing phase II double-blind, placebo-controlled trial that is assessing the efficacy and safety of cannabidivarin in Children With Autism Spectrum Disorder (ASD).