Tirzepatide is a first-in-class synthetic peptide that functions as a dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist. Engineered from a modified GIP sequence with GLP-1 receptor cross-reactivity, tirzepatide represents a fundamentally different approach from single-incretin therapies by simultaneously engaging both major incretin hormone pathways involved in metabolic regulation.
The dual mechanism produces complementary effects: GLP-1 receptor activation suppresses appetite, slows gastric emptying, and enhances insulin secretion, while GIP receptor activation improves fat metabolism, enhances insulin sensitivity in adipose tissue, and may contribute to preferential fat loss over lean mass. Together, these pathways create a more comprehensive metabolic intervention than either pathway alone.
In the landmark SURMOUNT and SURPASS clinical trial programs, tirzepatide demonstrated weight reductions of up to 22.5% of body weight at the highest doses — exceeding results from any single GLP-1 agonist in head-to-head comparisons. The SURPASS-2 trial directly showed superiority over semaglutide for both weight loss and glycemic control, establishing tirzepatide as the most effective incretin-based therapy currently available.
This compounded formulation delivers tirzepatide at 12.5mg/mL alongside pyridoxine (vitamin B6) at 50mg/mL via subcutaneous injection. The injectable route provides near-complete bioavailability, ensuring consistent therapeutic levels. High-dose B6 supports amino acid metabolism and neurotransmitter synthesis during the caloric deficit that accompanies treatment.
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