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*For medical professionals only
The results of a 12-week study of a novel oral non-peptide GLP-1RA in patients with type 2 diabetes reveal that
the 2022 European Association for the Study of Diabetes (EASD) Annual Meeting has come to a
successful conclusion.
This year's EASD brings us the latest progress in diabetes research, education, diagnosis and treatment technology, disease prevention, etc.
, as well as the latest research results
on hypoglycemic drugs.
Lilly & Company disclosed the results of a Phase 1 study of a non-peptide oral glucagon-like peptide-1 receptor agonist (GLP-1RA) LY3502970 (LY) during the meeting, which received widespread attention
.
Widely recognized, innovative drugs "new and new" GLP-1RA drugs appear in the public's field of vision as a new type of hypoglycemic drugs, it has a good hypoglycemic effect, can improve metabolic indicators, including weight loss and management of blood lipids and blood pressure, some GLP-1RA also has cardiovascular benefits, such multiple benefits have greatly helped
the comprehensive management of diabetes.
In recent years, with the increase of evidence-based medical evidence, the status of GLP-1RA in domestic and foreign guidelines has also been significantly improved [1,2], and its clinical application has become more and more and more and more recognized by clinicians and patients
.
However, at present, GLP-1RA used in our clinical practice in China is an injectable preparation, and it is a peptide drug, and there is no oral GLP-1RA.
For patients who reject injection regimens, the benefits of GLP-1RA remain somewhat impeded.
Regarding oral GLP-1RA, there have been certain breakthroughs
in recent years.
Oral GLP-1RA is made possible by co-formulation of semeglutide with sodium N-(8-[2-hydroxybenzoyl]-amino)octanoate (Salcaprozate Sodium, SNAC)[3].
。 However, experts such as Takahiro Kawai said: "The approved dose of oral semeglutide cannot achieve the high drug exposure required to be comparable to the hypoglycemic and weight-reducing effects observed with semeglutide injection [4]
.
" In addition, because drug absorption is significantly affected by food and fluids in the stomach [3], oral administration is limited to patients and requires patients to follow several steps, including drinking no more than approximately 120 mL of water while taking the drug and not eating, drinking, liquids, or other oral medications for at least 30 minutes after administration [5].
Such cumbersome requirements will have an impact
on patient treatment compliance.
As the exploration progressed, oral non-peptide GLP-1RA emerged, which was found to provide more standard drug formulations and simpler methods of administration [4], which is particularly beneficial
for patients with type 2 diabetes who require drug treatment.
Phase 1 results released: safe and effective blood sugar, significant weight loss LY3502970 is a novel, highly potent, oral, non-peptide GLP-1RA.
There are 5 cohorts
in the LY3502970 Phase 1 clinical study published in EASD.
Key inclusion criteria for the study included: patients aged 18-70 years, diagnosed type 2 diabetes ≥ 6 months, HbA1c ≥ 7.
0%, and ≤ 10.
5%.
These patients were randomized 3:1 to once-daily multiple-dose LY3502970 (n=51) or placebo (n=17) for 12 weeks
.
The baseline characteristics of each group are basically balanced
.
On the 84th day of treatment, the maximum plasma concentration (C max) ranged from 60 ng/mL to 236 ng/mL in the LY3502970 group, and the peak time of blood concentration (tmax) The median was 4~8 hours
.
On the 84th day of treatment, patients in the different doses of LY3502970 group decreased HbA1c by 1.
5%~1.
8% (placebo group decreased by 0.
4%), and lost 1.
6kg~5kg (placebo group gained weight by 0.
5kg).
In terms of safety, among patients treated with LY3502970, the most commonly reported adverse events in the treatment were nausea (47.
1%), decreased appetite (45.
1%), and vomiting (43.
1%)
.
These occur early in treatment and decrease
over time.
1 patient reported 2 serious gastrointestinal events (1 nausea and vomiting each); All other events were mild or moderate.
No clinically relevant liver abnormalities or serious adverse events
related to LY3502970 were reported.
This study shows that the new oral non-peptide GLP-1RA LY3502970 once-daily treatment shows comparable safety, potent hypoglycemic efficacy and significant weight loss effect as GLP-1RA injectable formulation
.
These data also support further clinical development
of the drug.
Summary:
The emergence of GLP-1RA has brought doctors and patients with type 2 diabetes a new treatment option that takes into account multiple benefits such as lowering blood sugar and weight loss, and has ushered in a new era
for diabetes treatment.
Now, the emergence of the new oral non-peptide GLP-1RA LY3502970 has brought another dawn to doctors and patients
.
It brings new hope
to patients with hypoglycemic needs, patients with weight loss needs, or patients who are unwilling or unable to inject treatment with GLP-1RA.
It is expected that future research will be further developed and bring more answers
.
Statement:
1.
Oral non-peptide GLP-1RA LY3502970 is an investigational drug that has not been approved in China, and related products or indications have not been listed globally
2.
Lilly does not recommend any unapproved drugs/indications
References:
[1] Diabetes Branch of Chinese Medical Association.
Guidelines for the prevention and treatment of type 2 diabetes mellitus in China (2020 edition)[J].
Chinese Journal of Diabetes.
2021; 13(4):315-409.
[2] American Diabetes Association.
Diabetes Care.
2021 Jan; 44(Suppl 1):S1-S232.
[3] Buckley ST,Bækdal TA,Vegge A,et al.
Transcellular stomach absorption of a derivatized glucagon-like peptide-1 receptor agonist.
Sci Transl Med.
2018; 10(467):eaar7047.
[4] Kawai T,Sun B,Yoshino H,et al.
Structural basis for GLP-1 receptor activation by LY3502970,an orally active nonpeptide agonist.
Proc Natl Acad Sci U S A.
2020; 117(47):29959-29967.
[5] Hedrington MS,Davis SN.
Oral semaglutide for the treatment of type 2 diabetes.
Expert Opin Pharmacother.
2019; 20(2):133-141.
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