Mavatrep
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Mavatrep (JNJ‐39439335) is a
TRPV1 The transient receptor potential cation channel subfamily V member 1 (TrpV1), also known as the capsaicin receptor and the vanilloid receptor 1, is a protein that, in humans, is encoded by the ''TRPV1'' gene. It was the first isolated member of th ...
receptor selective competitive antagonist. It is an investigational analgesic that may be a potential treatment for
analgesia Pain management is an aspect of medicine and health care involving relief of pain (pain relief, analgesia, pain control) in various dimensions, from acute and simple to chronic and challenging. Most physicians and other health professional ...
and/or
inflammation Inflammation (from la, inflammatio) is part of the complex biological response of body tissues to harmful stimuli, such as pathogens, damaged cells, or irritants, and is a protective response involving immune cells, blood vessels, and molec ...
. Phase I trials have been completed in healthy Japanese and Caucasian volunteers. Potential common
adverse effect An adverse effect is an undesired harmful effect resulting from a medication or other intervention, such as surgery. An adverse effect may be termed a " side effect", when judged to be secondary to a main or therapeutic effect. The term compl ...
s include thermohypoesthesia, chills, feeling cold, and feeling hot.


Pharmacokinetics

When administered orally once a day, mavatrep reached steady-state in healthy volunteers in approximately 14 days. It has a relatively long half life between 68 and 101 hours in Japanese subjects and between 82 and 130 hours in Caucasian subjects. Mavatrep is largely eliminated nonrenally. Mavatrep appears to be metabolized into two primary metabolites which are also eliminated nonrenally.


References

{{Reflist Ion channel blockers Analgesics Experimental drugs