Insights on LCMS Testing – Bioviridians

Insights on LCMS Testing

Expert guidance and analytical chemistry insights from Bioviridians’ professional team. Discover the latest techniques, best practices, and industry trends in LCMS testing for peptides, supplements, and biotech applications.

Semaglutide Overview

Semaglutide: Mechanism & Clinical Use

Semaglutide is a glucagon-like peptide-1 receptor agonist (GLP-1 RA) with a long elimination half-life, which allows it to be administered subcutaneously (sc) just once per week. Both the European Medicines Agency (EMA) and the U.S. Food and Drug Administration (FDA) have approved once-weekly sc semaglutide for the treatment of type 2 diabetes mellitus (T2DM).

Among currently available once-weekly GLP-1 RAs, semaglutide shows superior weight-loss effectiveness in patients with T2DM. It has also been evaluated as an anti-obesity medication in a phase II dose-finding study, where once-daily sc semaglutide produced greater weight loss than both placebo and once-daily 3.0 mg liraglutide in individuals with obesity but without T2DM. The amount of weight loss achieved exceeded the EMA and FDA requirements for anti-obesity drugs, and no major safety issues were observed. These results support the potential use of once-daily semaglutide as a future treatment for obesity.

Tirzepatide Overview

Tirzepatide (Mounjaro)

Tirzepatide (Mounjaro™) is a dual agonist that activates both the glucose-dependent insulinotropic polypeptide (GIP) receptor and the glucagon-like peptide-1 (GLP-1) receptor within a single molecule. GIP and GLP-1 are incretin hormones known for stimulating insulin secretion and suppressing glucagon release. Beyond this, GIP contributes to nutrient and energy metabolism, while GLP-1 slows gastric emptying, reduces appetite, and enhances satiety.

Eli Lilly is developing tirzepatide for multiple therapeutic areas, including type 2 diabetes mellitus (T2DM), obesity, cardiovascular disease in T2DM, heart failure, non-alcoholic steatohepatitis (NASH), obstructive sleep apnea, and reduction of obesity-related morbidity and mortality. In May 2022, tirzepatide received its first U.S. approval for improving glycemic control in adults with T2DM as an adjunct to diet and exercise.

Currently, tirzepatide is undergoing phase III clinical trials for heart failure, obesity, and cardiovascular complications in T2DM, and phase II development for NASH. This summary highlights the key milestones in tirzepatide’s development that led to its initial approval for treating T2DM.

PT-141 Overview

PT-141 (Bremelanotide)

PT-141 is a synthetic peptide analogue of α-MSH and functions as an agonist of melanocortin receptors—specifically MC3R and MC4R—which are primarily located in the central nervous system. In preclinical studies, administration of PT-141 to rats and nonhuman primates produced penile erections. In rats, systemic PT-141 also activated hypothalamic neurons, demonstrated by increased c-Fos immunoreactivity. Notably, neurons in this same hypothalamic region take up pseudorabies virus when it is injected into the corpus cavernosum, indicating a neural pathway relevant to erectile function.

Clinical studies in healthy men and in individuals with erectile dysfunction showed that PT-141 induces a rapid, dose-dependent increase in erectile activity. These findings support the potential of PT-141 as a promising therapeutic option for the treatment of sexual dysfunction.

BPC-157 Overview

BPC-157

BPC-157 is a 15–amino acid peptide with broad organ-protective properties demonstrated across numerous experimental models. Our study evaluated its effects on several key components of the healing process. The most critical factors in tissue repair— granulation tissue formation, angiogenesis, and collagen production—were specifically examined.

Using three rat models (skin incisional wounds, colon–colon anastomoses, and a synthetic sponge implantation model for angiogenesis), we investigated the impact of BPC-157 on granulation and collagen development, new blood vessel formation, and tensile strength. Histological assessments were performed to quantify collagen, reticulin fibers, and vascular structures through scoring and morphometric analysis.

Across all models, BPC-157–treated animals showed significant improvements compared with controls, demonstrating a strong healing-promoting effect. Notably, these benefits were observed regardless of the route of administration—including both intragastric and local delivery—highlighting BPC-157 as a promising therapeutic agent for tissue repair and regeneration.

References

REFERENCES

Seiwerth S., Sikiric P., Grabarevic Z., Zoricic I., Hanzevacki M., Ljubanovic D., Coric V., Konjevoda P., Petek M., Rucman R., Turkovic B., Perovic D., Mikus D., Jandrijevic S., Medvidovic M., Tadic T., Romac B., Kos J., Peric J., Kolega Z.
BPC-157’s Effect on Healing.
Molinoff P. B., Shadiack A. M., Earle D., Diamond L. E., Quon C. Y.
PT-141: A Melanocortin Agonist for the Treatment of Sexual Dysfunction.
Baker D. E., Walley K., Levien T. L.
Tirzepatide.
Volume 58, Issue 3.
(ORCID: 0000-0002-4605-3357, 0000-0001-5114-6067)
Christou G. A., Katsiki N., Blundell J., Fruhbeck G., Kiortsis D. N.
Semaglutide as a Promising Anti-Obesity Drug.
First published 15 February 2019.