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338

[Discussion] ATTAIN is doing more work than we give it credit for

Discussion Clean Column ×9

Something I keep coming back to: ATTAIN is doing more work than we give it credit for.

Oral semaglutide is a peptide co-formulated with an absorption enhancer and carries food and water timing requirements. A small molecule does not have that constraint, which is the practical distinction.

Analytically this is a small-molecule identity and purity problem, not a peptide one. The methods, the impurity classes and the reference standards are all different.

Milligram comparisons across molecule classes are meaningless. Potency is a property of the molecule at its receptor, not of the number on the label.

Ask me anything specific. Anything general I will probably get wrong.

464 up / 126 down79% upvoted30 commentsid 1vii1h12 Oct 2024

30 comments

21 in this archive, depth 6

best — the order this archive was captured in

u/tidy_vialdrawer_watch2868 points·1 year ago

The analytical point, which this board keeps getting wrong by importing habits from the peptide side.

For a peptide, purity is typically reported as area percent by HPLC with identity by mass spectrometry, and the impurity classes are things like deletion and oxidation products. For a small molecule the relevant impurities are synthetic intermediates, degradants and residual solvents, and identity is established differently.

So the certificate you would want looks different, the questions to ask are different, and a "purity" figure quoted here is not comparable to one quoted on the peptide boards. Anybody posting a result should say what method produced it, which is good practice everywhere and essential here.

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u/purity_pedantanalytical40 points·1 year ago

Spent an evening reading about small-molecule agonism at a peptide receptor. Genuinely interesting engineering.

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u/aksel_kjaer10 points·1 year ago

This. The absence of food and water timing restrictions is the practical difference people will actually notice.

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u/graph_it_gary27 points·1 year ago

Push back: daily dosing is not automatically better adherence. It is a different failure mode, not a solved problem.

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u/lukas_delgado6 points·1 year ago

Push back: daily dosing is not automatically better adherence.

Adding the standing caveat — unapproved, and research material is not for human use.

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u/zeynep_ndiaye8 points·1 year ago

nothing containing this is approved anywhere and research material is not for human use

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u/flair_enthusiast4 points·1 year ago

the tolerability profile reads broadly similar to the class

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u/yara_boateng3 points·1 year ago

Correction: that is the oral peptide product, which is a different thing entirely. This one is a small molecule.

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u/santiago_villalobos1 point·1 year ago

Careful — purity methods for peptides do not read across to a small molecule and the numbers are not equivalent.

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u/declared_value_dv5 points·1 year ago

the boards keep comparing it to injectables at matched doses, which is meaningless

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u/fasting_insulin_fOP3 points·1 year ago

Went looking for independent testing on this and found essentially nothing, which was clarifying.

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u/fabio_lehtinen1 point·1 year ago

nothing containing this is approved anywhere yet

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u/niels_norgaard1 point·1 year ago

small molecule, not a peptide, and that changes everything about it

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u/kenji_kimani1 point·1 year ago

What analytical method was used — this is not the usual peptide assay question?

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u/kenji_laurent4 points·1 year ago

Disagree. You are comparing doses across a small molecule and a peptide, which is not a comparison of anything.

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u/ayesha_erdogan-8 points·1 year ago

a non-peptide agonist does not degrade the way a peptide does

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u/yara_boateng19 points·1 year ago

Daily dosing gives a very different exposure profile from a weekly injectable: peaks and troughs within each day rather than a smoothed weekly curve.

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u/fasting_insulin_fOP15 points·1 year ago

Daily dosing gives a very different exposure profile from a weekly injectable: peaks and troughs within each day rather than a smoothed weekly curve.

Disagreeing with this bit: daily dosing is a different adherence problem, not a better one.

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u/nils_ferreira10 points·1 year ago

Small fix — the two programme names got swapped upthread and it changes which population the figure came from.

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u/clara_weiss3 points·1 year ago

identity testing on a small molecule is a different analytical problem

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u/whois_wanda3 points·1 year ago

ATTAIN and ACHIEVE are the programmes to keep straight

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The small-molecule oral: why a non-peptide agonist escapes the absorption problems of oral semaglutide, what the ATTAIN and ACHIEVE readouts showed, and what a pill with no refrigeration requirement would do to the entire supply conversation this site is built around.

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