СHR is a first-in-class analgesic drug with a novel mechanism of action – agonist of cannabinoid CB1 receptors and dopaminergic D1 and D3 receptors. At the same time, CHR is not a structural analog of the known cannabinoids and doesn’t have psychotropic adverse effects, inherent in them.
Dosage form – solid dosage forms (tablets or capsules) for oral use. Prototypes of injectable dosage forms are developed.
Patent profile: patented in Russia, EAEU, USA, EU, China.
Indications for use: Thanks to its pharmacological properties and safety advantages over narcotic and non-narcotic analgesics, CHR may be used for the following indications:
– treatment of chronic pain syndrome in cancer patients as monotherapy at the first stage and in combination with oral opioid analgesics at the second – third stages of pain management;
– treatment of pain syndrome in non-cancer patients (including those in palliative care) who can’t be treated with opioid analgesics;
– combined treatment of neuropathic pain syndrome of any origin (including phantom pains) when there is a need for long-term analgesic therapy with minimal side effects and avoiding the problems of prescribing opioids.
Main advantages:
– High efficacy at low doses (oral ED50 in rodents – 5 mg/kg), comparable to that of the opioid tramadol in 20 mg/kg dose; expected single oral dose in humans – 5-10 mg;
– Prolonged analgesic action – up to 24 hours after single use:
– Low toxicity: LD50 is over 1500 mg/kg (oral, rodents);
– High therapeutic index (LD50/ED50 ratio) – much higher than that of known analgesics, which eliminates the risk of dangerous overdoses;
– Absence of side effects inherent in narcotic analgesics (addiction, withdrawal syndrome, psychotropic effects, respiratory depression, gastrointestinal problems).
Current status: Laboratory technology of substance synthesis is developed. Prototype dosage form is developed. The mechanism of action is confirmed, data on the absence of psychotropic effects is obtained, preclinical studies of efficacy (in models of pain syndrome) and safety (general toxicity) are partially completed.