Leptin is a 167 amino acid peptide with a 21-amino acids secretory signal sequence. Leptin plays key roles in the regulation of neuroendocrine function and energy homeostasis. The blood levels of leptin mirror energy stores, fat mass, or energy deficiency.
Leptin therapy is effective in certain cardiometabolic disorders related to leptin deficiency, but not in normal obesity.
Leptin for Therapeutic Use
Recombinant Methionyl-human Leptin (r-Met-hu-leptin)
Metreleptin (Myalept) is a recombinant human leptin (r-Met-hu-leptin) analog, in which a methionine residue has been added to the amino terminus to improve productivity and molecular folding. The r-Met-hu-leptin analog is a nonglycosylated polypeptide consisting of 147 amino acids with a disulfide bond between Cys-97 and Cys-147. Metreleptin is produced by Escherichia coli (E. coli). It was developed by Amgen and granted approval by the FDA in the USA, the EMA in Europe and the PMDA in Japan.
As Metreleptin has a reported average terminal half-life of about 4 h in humans, daily administration is needed to maintain blood concentrations.
Pegylated Human Leptin
To design long-acting leptin, polyethylene glycol (PEG) is linked to human recombinant leptin. The conjugated protein PEG-OB has a longer half-life (> 48 h). Recombinant human leptin is expressed and purified from E. coli, and then chemically linked to PEG with an average molecular weight of 42 kDa in a 1:1 ratio.
Yaohai Bio-Pharma Offers One-Stop CDMO Solution for Recombinant Leptin
Leptin Pipelines
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Generic name
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Brand Name/Altermative Name
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Expression System
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Indications
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Manufacturer
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R&D Stage
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Metreleptin
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Myalepta, AC-164594, KTR-103, Myalept, メトレレプチン
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Escherichia coli (E. coli)
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Familial focal lipodystrophy, amenorrhoea
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Amryt Pharmaceuticals DAC, Amryt Pharma Plc, Shionogi & Co., Ltd.
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Approved
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Recombinant methionyl human Fc-leptin
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LEPTIN A-200
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Pending Update
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Obesity
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Amgen, Inc.
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Clinical trial
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CV-08-01
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CP-deltaSOCS3、CV-08、CP-SP
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Pending Update
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Obesity
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Cellivery Therapeutics, Inc.
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Pre-clinical
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BL-5040
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Leptin variant
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Pending Update
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Inflammatory Bowel Disease
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BioLineRx, Yissum
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Pre-clinical
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