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When administered, the compound binds to both receptor types, triggering enhanced insulin secretion from pancreatic beta cells while simultaneously suppressing inappropriate glucagon release

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However, tesofensine faces significant challenges - cardiovascular side effects (increased heart rate and blood pressure) raised safety concerns, FDA has not approved it despite promising efficacy data, development stalled after Phase 3 trials, currently available only through research chemical suppliers with questionable legality, and the stimulant-like mechanism creates dependency and tolerance risks not seen with GLP-1 agonists