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Showing 1 - 10 of 35 results

Status:
US Approved Rx (2015)
First approved in 2015

Class (Stereo):
CHEMICAL (ABSOLUTE)



Rolapitant (VARUBI) is neurokinin 1 (NK1) receptor antagonist. Rolapitant does not have significant affinity for the NK2 or NK3 receptors. Drug is indicated in combination with other antiemetic agents in adults for the prevention of delayed nausea an...
Status:
US Approved Rx (2018)
First approved in 2014

Class (Stereo):
CHEMICAL (ACHIRAL)



Fosnetupitant is a prodrug form of netupitant. Netupitant is a selective antagonist of human substance P/neurokinin 1 (NK-1) receptors. Upon intravenous administration, fosnetupitant is converted by phosphatases to its active form. It competitively b...
Status:
US Approved Rx (2008)
First approved in 2003

Class (Stereo):
CHEMICAL (ABSOLUTE)



Fosaprepitant (Emend for Injection (US), Ivemend (EU)) is a prodrug of Aprepitant. Once biologically activated, the drug acts as a substance P/neurokinin 1 (NK1) receptor antagonist which, in combination with other antiemetic agents, is indicated for...
Status:
Investigational

Class (Stereo):
CHEMICAL (ABSOLUTE)



AV608, a 4-aminopiperidine derivative, is a selective, specific, long-acting, orally active and potent nonpeptidic antagonist of the NK-1 receptor. AV-608 had been in phase II clinical trials for the treatment of social phobia and overactive bladder ...
Status:
Investigational

Class (Stereo):
CHEMICAL (ABSOLUTE)



Nolpitantium (SR-140333) is a highly selective nonpeptide antagonist of neurokinin-1 (NK1) receptor. Nolpitantium potently, selectively and competitively inhibited substance P binding to NK1 receptors from various animal species, including humans. I...
Status:
Investigational

Class (Stereo):
CHEMICAL (ABSOLUTE)



Orvepitant is a novel generation brain penetrant, selective and potent, small molecule NK-1 receptor antagonist. Orvepitant’s (GW823296) mode of action and developability characteristics made it a suitable development candidate for the treatment of c...
Status:
Investigational

Class (Stereo):
CHEMICAL (ACHIRAL)


Tradipitant is a neurokinin 1 receptor antagonist. The dose of 50 mg of tradipitant given orally for 4 weeks was not superior to placebo in reducing itch intensity in patients with atopic dermatitis. However, in a subsequent study, in which a higher ...
Status:
Investigational

Class (Stereo):
CHEMICAL (ABSOLUTE)



Talnetant (SB-223412) is a selective, orally active neurokinin 3 receptor antagonist and is under development for the potential treatment of several disorders, including irritable bowel syndrome, schizophrenia, chronic obstructive pulmonary disease, ...
Status:
Investigational

Class (Stereo):
CHEMICAL (ACHIRAL)


Befetupitant (Ro67-5930) is a high-affinity, competitive, tachykinin 1 receptor (NK1R) antagonist that was initially invented by Hoffmann-La Roche as a potential antiemetic drug. These studies were discontinued, because of the clinical trials with th...