ESPEYB17 14. The Year in Science and Medicine (1) (16 abstracts)
14.12. Brain-Sparing sympathofacilitators mitigate obesity without adverse cardiovascular effects
Mahú I , Barateiro A , Rial-Pensado E , Martinéz-Sánchez N , Vaz SH , Cal PMSD , Jenkins B , Rodrigues T , Cordeiro C , Costa MF , Mendes R , Seixas E , Pereira MMA , Kubasova N , Gres V , Morris I , Temporão C , Olivares M , Sanz Y , Koulman A , Corzana F , Sebastião AM , López M , Bernardes GJL & Domingos AI
To read the full abstract: Cell Metab. 2020 Jun 2;31(6):1120-1135.e7. doi: 10.1016/j.cmet.2020.04.013.
This experimental rodent study of a PEGylated amphetamine (PEGyAMPH) designed to not cross the blood brain barrier is interesting for 2 reasons. First, it shows that its peripheral anti-obesity effects alone (without the central anorexic effects of amphetamine) are sufficient to achieve weight loss by acting on the β2-adrenoceptor to increase lipolysis and thermogenesis. Second, it shows that the cardiac side effects of amphetamine are mediated by central, instead of direct peripheral, signaling.
Since the 1930’s, amphetamine-class medications have been widely used to treat obesity, although cardiovascular safety concerns have led to repeated bans. ‘Rainbow diet pills’ combined an amphetamine and other agents to block its peripheral stimulant effects, however, these were banned in the 1960’s, and again in the 2000’s shortly after their re-emergence in North America. Phentermine, an amphetamine derivative, has been used in obesity since the 1960’s; its combination with fenfluramine (Phen-Fen) was withdrawn in 1997 due to cases of cardiac valve disease; however, its combination with topiramate remains FDA-approved since 2012 (although not approved in Europe).
There is a very long history of anti-obesity medications that have been withdrawn even several years after their approval, as long-term safety issues became apparent. Many agents are clearly effective to produce weight loss, but long-term safety concerns seem to arise repeatedly, not only for amphetamines. Lorcaserin, a centrally acting 5-HT2C receptor agonist approved by the FDA in 2012 (but not in Europe), was the latest casualty, being withdrawn in the US in February 2020 due to increased risks of pancreatic, colorectal and lung cancers.
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ESPE Yearbook of Paediatric Endocrinology
ISSN 1662-4009 (Online)
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