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c/glp1science·posted 2 years ago by u/swirl_dont_shake

someone explain incretin to me like I have not read a paper in years

Needs Source Clean Column ×8 Slow Clap ×1 Well Actually ×3

someone explain incretin to me like I have not read a paper in years. Searched first, found three threads that contradict each other, hence the post.

GLP-1 receptor agonism acts both peripherally — insulin secretion in a glucose-dependent way, slowed gastric emptying — and centrally, on appetite regulation. The central component is the better explanation for sustained intake reduction.

Why mechanism talk keeps misleading people, including me.

A mechanism tells you a direction. It does not tell you a magnitude, a timescale, or whether the pathway is operative at the exposures involved. "Receptor X is expressed in tissue Y" is a fact; "therefore effect Z in a person" is a hypothesis with several missing steps.

The corrective is boring and it works: ask whether the evidence is preclinical or human, ask what exposure was used, and read the limitations section before the abstract. Most of the confidently wrong posts on this board — several of them mine — skipped all three.

The GIP question, which is the most interesting unsettled thing in this field.

Dual agonism at GIP and GLP-1 receptors produces clinical results that are robust and well replicated. What is not settled is the mechanism by which the GIP arm contributes — there is a genuine scientific argument about agonism versus antagonism at that receptor, with reasonable people and real data on both sides.

It is worth sitting with that. The clinical effect is not in doubt; the explanation is. That is an ordinary state of affairs in pharmacology and it is a good corrective to the confident mechanistic stories that circulate here.

That is everything I have. The rest is opinion and I have tried to keep it out.

4,627 up / 547 down89% upvoted32 commentsid 1xplz911 Mar 2024

32 comments

21 in this archive, depth 4

best — the order this archive was captured in

u/enzo_danquah637 points·2 years ago

Tolerance to the gastric effect develops with continued exposure while the appetite effect largely persists. That single fact explains most of the "it settles but it still works" pattern the side-effect board reports.

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u/annika_fonseca399 points·2 years ago

What was the exposure in that experiment relative to therapeutic?

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u/milos_vanhecke601 points·2 years ago

Went looking for human data on a mechanism everybody here asserts. Found preclinical work and one small study. That was clarifying.

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u/emil_agyeman505 points·2 years ago

Went looking for human data on a mechanism everybody here asserts.

Adding the caveat the paper itself makes in its limitations section, which is stronger than anything in this thread.

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u/swirl_dont_shakeOPreconstitution308 points·2 years ago

Adding the caveat the paper itself makes in its limitations section, which is stronger than anything in this thread.

Disagreeing with this specific inference — that is a preclinical result being read as human pharmacology.

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u/ferran_batista241 points·2 years ago

the peripheral and central stories are not in competition

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u/wholesome_lurker404 points·2 years ago·edited

Read the primary paper after arguing about the summary for a fortnight. The discussion section said almost the opposite of what the thread had concluded.

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u/swirl_dont_shakeOPreconstitution193 points·2 years ago·edited

Was completely wrong about the gastric emptying story in a thread here two years ago. Someone corrected me with a citation and I have not made that mistake since.

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u/vomit_free_since147 points·2 years ago

Was completely wrong about the gastric emptying story in a thread here two years ago.

swirl_dont_shake is right that mechanism gives direction and not magnitude. Worth pinning.

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u/employer_carveout298 points·2 years ago

What does the discussion section say about the limitation you are glossing?

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u/aleksi_eriksen136 points·2 years ago

Correction: that is glucose-dependent insulin secretion, which is why hypoglycaemia risk is low as monotherapy. Not the same claim as you made.

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u/employer_carveout90 points·2 years ago

Careful — you have a plausible mechanism and no evidence that it is the operative one in the case you are describing.

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u/priya_guerrero70 points·2 years ago

mechanism explains a direction, not a magnitude

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u/greta_lokken25 points·2 years ago

Receptor expression in a tissue is necessary but not sufficient for an effect. You also need the agonist to reach it at relevant exposure, and that is where a lot of confident mechanism talk falls down.

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u/dose_creep_dan129 points·2 years ago

The mental model, in four steps, that makes the rest of this site legible.

One: gut hormones amplify the insulin response to food. Two: agonists at those receptors act peripherally on insulin secretion and gastric emptying, and centrally on appetite. Three: structural modification gives them a long half-life, so exposure is smooth and weekly. Four: tolerance develops to some effects and not to others.

From those four, most of what the experience boards report falls out: why the side effects cluster early, why they settle at a stable dose, why appetite reduction persists, and why the scale and the appetite move on different clocks.

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u/hassan_ostergaard45 points·2 years ago

The half-life explanation was the thing that made weekly dosing intuitive for me rather than arbitrary.

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u/swirl_dont_shakeOPreconstitution152 points·2 years ago

Started reading limitations sections first. It has changed how much weight I give to almost everything posted here.

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u/bastian_eriksen39 points·2 years ago·edited

Started reading limitations sections first.

This is the concept everything else on this board is downstream of.

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u/yusuf_ramos26 points·2 years ago

Push back: a receptor being expressed in a tissue does not tell you the agonist reaches it at therapeutic exposure.

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u/gastric_emptying_gMOD76 points·2 years ago

Left up and flaired Explainer. This is the standard of post the board was created for.

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u/nora_lundgren-27 points·2 years ago

dose response is not linear and nobody should assume it is

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The mechanism layer: incretin physiology, receptor distribution, gastric emptying, central appetite signalling, glucagon-receptor contribution, amylin co-agonism, and the pharmacokinetics that make weekly dosing possible. Papers get cited by journal and year or they get a [needs source] reply.

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