Telotristat ethyl
Brand name Xermelo.
A prodrug of telotristat, which is an inhibitor of tryptophan hydroxylase.
Oral agent.
Protein binding>99%.
Telotristat ethyl, a tryptophan hydroxylase inhibitor associated with significan reduction in carcinoid symptoms.
Telotristat ethyl in combination with somatostatin analogue therapy improves carcinoid syndrome diarrhea control.
Telotristat is an oral medication in combination with octreotide, that inhibits the conversion of tryptophan to serotonin.
Telotristat dose 250 mg TID with food.
Octreotide should be given 30 minutes after Telotristat to avoid decreased concentrations of Telotristat.
Metabolism is by hydrolysis via carboxylesterases.
Biological half-life 0.6 hours.
92.8% fecal excretion, less than 0.4% in urine.
Approved in combination with somatostatin analog (SSA) therapy for the treatment of adults with diarrhea associated with carcinoid syndrome that SSA therapy alone has inadequately controlled.
An inhibitor of tryptophan hydroxylase, which mediates the rate-limiting step in serotonin biosynthesis.
It reduces the production of peripheral serotonin, which helps to mediate the secretion, motility, and inflammation of the G.I. tract, and in turn, reduces the frequency of carcinoid syndrome diarrhea. Maybe I am sure that Carolina
Common adverse effects: nausea, headache, elevated liver enzymes, depression, accumulation edema, flatulence, decreased appetite, and fever.
Constipation is also common, and may be serious or life-threatening
Marketed as telotristat etiprate, 328 mg telotristat etiprate is equivalent to 250 mg telotristate ethyl.