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| Clinical data | |
|---|---|
| Trade names | Symlin |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a605031 |
| Routes of administration | Subcutaneous |
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| Pharmacokinetic data | |
| Bioavailability | 30 to 40% |
| Protein binding | ~60% |
| Metabolism | Renal |
| Eliminationhalf-life | ~48 minutes |
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| Chemical and physical data | |
| Formula | C171H267N51O53S2 |
| Molar mass | 3949.44 g·mol−1 |
| 3D model (JSmol) | |
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Pramlintide (trade nameSymlin) is an injectableamylin analogue drug fordiabetes (both type 1 and 2), developed byAmylin Pharmaceuticals (now a wholly owned subsidiary ofAstraZeneca).[1] Pramlintide is sold as an acetate salt.
Pramlintide is an analogue ofamylin, a small peptidehormone that is released into thebloodstream by theβ cells of thepancreas along withinsulin after a meal.[2] Like insulin, amylin is completely absent in individuals with Type I diabetes.[3]
In synergy with endogenous amylin, pramlintide aids in the regulation of bloodglucose by slowinggastric emptying, promotingsatiety viahypothalamic receptors (different receptors than forGLP-1), and inhibiting inappropriate secretion ofglucagon, a catabolic hormone that opposes the effects of insulin and amylin. Pramlintide also has effects in raising the acute first-phase insulin response threshold following a meal.[citation needed]
Both a reduction inglycated hemoglobin and weight loss have been shown in insulin-treated patients with type 2 diabetes taking pramlintide as an adjunctive therapy.[4]
In the research field, pramlintide has been experimented with and used as a potential treatment drug. Pramlintide has demonstrated its ability to decreaseamyloid beta plaques inAlzheimer's disease mouse models.[5]
Pramlintide has been approved on 3/16/2005 by the FDA, for use by type 1 and type 2 diabetic patients who use insulin.[6](subscription required) Pramlintide allows patients to use less insulin, lowers average blood sugar levels, and substantially reduces what otherwise would be a large unhealthy rise in blood sugar that occurs in diabetics right after eating.
Apart from insulin analogs, pramlintide is the only drug approved by the FDA to lower blood sugar in type 1 diabetics since insulin in the early 1920s.[citation needed][7]
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Since native human amylin is highlyamyloidogenic and potentially toxic, the strategy for designing pramlintide was to substitute residues from rat amylin, which is less amyloidogenic[8][9] but presumably retains clinical activity. Proline residues are known to be structure-breaking[clarification needed] residues, so these were directly grafted into the human sequence. Despite its enhanced stability compared to human amylin, however, pramlintide is still able to organize into amyloid material.[10]
Amino acid sequences:
| Pramlintide | KCNTATCATQRLANFLVHSSNNFGPILPPTNVGSNTY-(NH2) |
| Amylin | KCNTATCATQRLANFLVHSSNNFGAILSSTNVGSNTY-(NH2) |
| Rat amylin | KCNTATCATQRLANFLVRSSNNLGPVLPPTNVGSNTY-(NH2) |
Pramlintide is apositively charged protein.[citation needed]