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improving safety profiles with prodrug constructs that functionalize the C-3 hydroxyl group with hydrophilic moieties (e.g., like PEG/amino acids), expand therapeutic windows, e.g., prodrug derivatives that increase HepG2 IC 50 from 22.5 M to 58.3 M (Tao et al., 2015)
The only persistent side effect was appetite suppression, which is the intended therapeutic outcome
Additionally, the lysine at position 28 is substituted with arginine, leaving the lysine at position 26 available for attachment to a fatty-acid/ethylene glycol-like chain , which extends the drugs half-life by binding to serum albumin (Figure 1)
"Wegovy injections are considered slightly more effective than the tablet," says Bradshaw
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