Delving into the Latest Updates on MK-0999 with Synapse

Overview

Basic Info

Drug Type

Chemical drugs, Diagnostic radiopharmaceuticals

Synonyms

F18 labeled MK-0999

Target-

Action-

Mechanism-

Therapeutic Areas

Other Diseases

Active Indication-

Inactive Indication

Chemotherapy-induced nausea and vomiting

Originator Organization

Merck Sharp & Dohme Corp.

Active Organization-

Inactive Organization

Merck Sharp & Dohme Corp.

License Organization-

Drug Highest PhasePendingPhase 1

First Approval Date-

Regulation-

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The type 1 neurokinin receptor (NK1R) antagonist aprepitant and its i.v. prodrug fosaprepitant have been approved for prevention of acute and delayed nausea and vomiting associated with chemotherapy. This study evaluated the magnitude and duration of brain NK1R occupancy over a period of 5 days after single-dose i.v. infusion of 150-mg fosaprepitant and single-dose oral administration of 165-mg aprepitant, using serial [(18)F]MK-0999 positron emission tomography (PET) in 16 healthy subjects. Each subject underwent three scans. Brain NK1R occupancy rates after i.v. fosaprepitant at time to peak concentration (T(max); ~30 min), 24, 48, and 120 h after the dose were 100, 100, ≥97, and 41-75%, respectively. After aprepitant, NK1R occupancy rates at these time points (T(max) ~4 h) were ≥99, ≥99, ≥97, and 37-76%, respectively. Aprepitant plasma concentration profiles were comparable for the two dosage forms. The study illustrates the utility of PET imaging in determining central bioequivalence in a limited number of subjects.

100 Deals associated with MK-0999

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Chemotherapy-induced nausea and vomiting	Phase 1	-	Merck Sharp & Dohme Corp.	01 Apr 2010

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01111851 (0869-183, CTgov)	Phase 1	Chemotherapy-induced nausea and vomiting	16	Ondansetron+Dexamethasone+MK0999+Fosaprepitant 150 mg (Fosaprepitant 150 mg)	xqypdhsvni(erbnwxspnu) = hxtsxdmpxu ztflceuurp (myfdmosisi, edvdywzxlg - sbylqsyaor) View more	-	03 Nov 2011
				Ondansetron+Dexamethasone+MK0999+Aprepitant 165 mg (Aprepitant 165 mg)	xqypdhsvni(erbnwxspnu) = qwnaumbugo ztflceuurp (myfdmosisi, grxeilvboo - zmdpnlhmlo) View more