Tecosactide is a synthetic 24-peptide corticotropin analogue. The amino acid sequence is identical to the 24 amino acids of the amino-terminal of natural corticotropin (human, bovine and porcine), and it has the same physiological activity as natural ACTH. “It is characterized by the absence of antibody reactions, generally without serious side effects, and is especially suitable for patients who have allergic reactions or are ineffective to natural porcine corticotropin.”
“It induces adrenal hyperplasia, stimulates the secretion of adrenocortical hormones, especially (cortisol) and some mineralocorticoids such as corticosterone, and also stimulates the secretion of androgens, but with a weaker effect.”
There was little effect on aldosterone secretion. The half-life is 3 hours. In 2008, the FDA approved Tecokotide from Novartis for the diagnosis of adrenal insufficiency. It is currently being studied at RandboudUniversity for the treatment of idiopathic membranous nephropathy.
The whole liquid phase synthesis method is the synthesis method of ticacotide. This method has many steps, long synthesis time, and requires expensive catalysts and high-pressure equipment, which has the disadvantages of high cost, many impurities, operation danger, and low yield. It has been reported that synthesis one by one using the Z-protection strategy, in which hydrogenation is used to remove the protective base at each step, has long steps, cumbersome operation, high cost and low yield. Serine is prone to racemization due to one-to-one coupling during purification, which is difficult to purify.
“Like adrenocorticotropic hormone, ticcotide stimulates the secretion of cortical hormones (mainly cortisol) from the adrenal cortex.” Therefore, there was no effect in patients with severe adrenocortical dysfunction.
Ticocotide is a synthetic polypeptide consisting of 24 amino acids. It is identical in structure to the first to the 24th amino acids of ACTH. Intravenous administration rapidly increases blood cortisol levels. A continuous intravenous drip should be used to maintain blood cortisol concentrations. For intramuscular injection, serum cortisol reached its peak at 1h after injection. After that, elevated cortisol can be maintained for approximately 24 hours.
Post time: Jun-28-2023