Bivamelagon: Molecular Structure
Chemical properties, amino acid sequence, and structural analysis
📌TL;DR
- •Molecular formula: C35H53ClN4O4
- •Molecular weight: 629.3 Da
- •Half-life: Not publicly disclosed (supports once-daily oral dosing)
Amino Acid Sequence
43 amino acids
Formula
C35H53ClN4O4
Molecular Weight
629.3 Da
Half-Life
Not publicly disclosed (supports once-daily oral dosing)
Molecular Structure#
Bivamelagon is a non-peptide small molecule, not a peptide. It is orally bioavailable and designed to cross the blood-brain barrier to reach MC4R in the hypothalamus. The molecule was developed by LG Chem and licensed to Rhythm Pharmaceuticals.
Key Molecular Features#
| Feature | Description |
|---|---|
| Molecular type | Non-peptide small molecule |
| Target receptor | Melanocortin-4 receptor (MC4R) |
| Route | Oral (daily tablet) |
| CNS penetration | Sufficient to reach hypothalamic targets |
| Selectivity | MC4R agonist (selectivity profile not fully disclosed) |
| Developer | LG Chem (licensed to Rhythm Pharmaceuticals) |
MC4R Receptor Pharmacology#
The melanocortin-4 receptor is a G-protein-coupled receptor (GPCR) in the hypothalamus that is central to appetite regulation and energy homeostasis. Activation of MC4R by its natural ligand alpha-MSH suppresses appetite and increases energy expenditure. Bivamelagon mimics this activation pharmacologically.
Comparison with Setmelanotide#
| Property | Bivamelagon | Setmelanotide |
|---|---|---|
| Type | Small molecule | Cyclic peptide |
| Route | Oral daily | SC daily injection |
| MC4R selectivity | Under characterization | MC4R selective |
| CNS penetration | Oral with BBB penetration | Peripheral then CNS |
| Indication | Hypothalamic obesity | Genetic obesity (POMC, PCSK1, LEPR) |
Pharmacokinetic Properties#
| Parameter | Value |
|---|---|
| Administration | Oral daily tablet |
| Half-life | Not publicly disclosed |
| Bioavailability | Oral (sufficient for daily dosing) |
| BBB penetration | Confirmed by clinical CNS effects |
Molecular Context#
Bivamelagon belongs to the Metabolic category of research peptides. The molecular properties of Bivamelagon determine its pharmacological behavior, including receptor binding, distribution, metabolism, and elimination. Understanding these properties is fundamental to interpreting clinical data and designing research protocols.
Structural Overview#
Bivamelagon is characterized as: Bivamelagon (LB54640) is a non-peptide small molecule agonist of the melanocortin-4 receptor (MC4R). Unlike setmelanotide (a cyclic peptide), bivamelagon is an orally bioavailable synthetic compound with sufficient CNS penetration to activate hypothalamic MC4R. The exact chemical structure has not been publicly disclosed..
Amino Acid Sequence Details#
The amino acid sequence of Bivamelagon is: Not applicable (non-peptide small molecule). This sequence determines the peptide's three-dimensional structure, receptor binding properties, and biological activity.
Pharmacokinetic Profile#
Half-Life: Not publicly disclosed (supports once-daily oral dosing)
The half-life of a peptide influences dosing frequency, duration of effect, and the clinical utility of the compound. Researchers should consider the half-life when designing experimental protocols.
Related Reading#
Frequently Asked Questions About Bivamelagon
What type of peptide is Bivamelagon?
Bivamelagon (LB54640) is an oral small molecule melanocortin-4 receptor (MC4R) agonist developed by Rhythm Pharmaceuticals (licensed from LG Chem) for hypothalamic obesity in patients aged 12 and older. In a Phase 2 trial, bivamelagon achieved 9.3% BMI reduction at 600 mg and 7.7% at 400 mg over 14 weeks, with significant hunger score reductions. It is the first oral MC4R agonist in clinical development for this rare obesity indication.
What is the half-life of Bivamelagon?
The reported half-life of Bivamelagon is Not publicly disclosed (supports once-daily oral dosing). Half-life can vary depending on the route of administration, formulation, and individual factors. This information is based on available preclinical or pharmacokinetic data.
What is the amino acid sequence of Bivamelagon?
The amino acid sequence of Bivamelagon is Not applicable (non-peptide small molecule). Bivamelagon (LB54640) is a non-peptide small molecule agonist of the melanocortin-4 receptor (MC4R). Unlike setmelanotide (a cyclic peptide), bivamelagon is an orally bioavailable synthetic compound with sufficient CNS penetration to activate hypothalamic MC4R. The exact chemical structure has not been publicly disclosed.. This sequence determines its biological activity and binding properties.
How stable is Bivamelagon in storage?
Bivamelagon is typically supplied as a lyophilized powder for maximum stability. Bivamelagon (LB54640) is a non-peptide small molecule agonist of the melanocortin-4 receptor (MC4R). Unlike setmelanotide (a cyclic peptide), bivamelagon is an orally bioavailable synthetic compound with sufficient CNS penetration to activate hypothalamic MC4R. The exact chemical structure has not been publicly disclosed.. When reconstituted, it should be stored refrigerated at 2-8 degrees C and protected from light. Lyophilized powder should be stored at -20 degrees C.
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