Effect of oral semaglutide on the pharmacokinetics of thyroxine after dosing of levothyroxine and the influence of co-administered tablets on the pharmacokinetics of oral semaglutide in healthy subjects: an open-label, one-sequence crossover, single-center, multiple-dose, two-part trial

Hauge, Camilla; Breitschaft, Astrid; Hartoft‐Nielsen, Marie‐Louise; Jensen, Simon; Bækdal, Tine A.

doi:10.1080/17425255.2021.1955856

“…After treatment, serum Tg and TgAb levels in both groups decreased, and the control group had lower results than the observation group, suggesting that levothyroxine tablets combined with iodine-131 could eliminate normal follicular cells and reduce the synthesis and level of Tg, thereby reducing antigen stimulation and TgAb level. This is consistent with the research results by Liang [ 20 , 21 ]. In addition, there was no significant difference in the adverse reactions of the two groups of patients, which indicated that levothyroxine tablets combined with iodine-131 would not increase the adverse reactions of thyroid cancer patients.…”

Section: Discussionsupporting

confidence: 94%

Effectiveness and Safety of Levothyroxine Tablets Combined with Iodine-131 in the Treatment of Thyroid Cancer

Bai

¹

,

Jin

²

,

Liu

³

et al. 2022

Journal of Oncology

1

0

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Objective. To explore the effectiveness of levothyroxine tablets combined with iodine-131 in thyroid cancer patients after radical thyroidectomy and the effect on their serum thyroglobulin (Tg) and thyroglobulin antibody (TgAb) levels. Methods. A total of 70 thyroid cancer patients receiving radical thyroidectomy in our hospital from July 2015 to April 2016 were recruited and were assigned via different treatment methods (1 : 1) to receive either levothyroxine tablets (observation group) or levothyroxine tablets plus iodine-131 (control group). Outcome measures included treatment efficiency, 1, 3, and 5-year recurrence and metastasis, serum Tg and TgAb levels, postoperative survival, and adverse reactions. Results. The total effective rate of treatment in the control group was significantly higher than that in the observation group ( P < 0.05 ). There was no significant difference in cancer recurrence and metastasis rate between the two groups one year postoperatively ( P > 0.05 ). The rate of cancer recurrence and metastasis in the control group was significantly lower than that in the observation group 3 and 5 years after surgery ( P < 0.05 ). Before treatment, there was no significant difference in serum Tg and TgAb levels between the two groups ( P > 0.05 ). After treatment, serum Tg and TgAb levels decreased in both groups, with lower results in the control group ( P < 0.05 ). There was no significant difference in the 1 and 3-year survival rates between the two groups ( P > 0.05 ). The 5-year survival rate in the control group was significantly higher than that in the observation group ( P < 0.05 ). There was no significant difference in adverse reactions between the two groups ( P > 0.05 ). Conclusion. Levothyroxine tablets combined with iodine-131 for thyroid cancer patients undergoing radical thyroidectomy effectively could improve the treatment efficiency, reduce the risk of cancer recurrence and metastasis after surgery, lower the serum Tg and TgAb levels of patients, and prolong the survival of patients, with a high safety profile. Further trials are, however, required prior to clinical promotion.

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“…The synthetic levothyroxine it contains is identical to the thyroxine naturally secreted by the thyroid gland and is converted to T3 in peripheral organs, which then exerts its specific effects by binding to T3 receptors [ 16 ]. The main component of levothyroxine sodium tablets is levothyroxine, and the binding rate to specific transporters is extremely high, about 99.97% [ 17 ]. The binding of this protein to hormones is not a covalent structure, so the plasma concentrations of bound and free hormones can be continuously and rapidly exchanged to maintain the physiological function of the thyroid, inhibit TSH secretion, reduce tumor cell adhesion, and promote the body's immunomodulatory effects [ 12 , 13 ].…”

Section: Introductionmentioning

confidence: 99%

Clinical Efficacy of Levothyroxine Sodium plus I 131 in the Treatment of Patients with Thyroidectomy and Its Effect on the Levels of Thyroglobulin and Thyrotropin

Pang

¹

,

Wang²,

Cheng

³

2022

Evidence-Based Complementary and Alternative Medicine

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Objective. This study was to evaluate the clinical efficacy of levothyroxine sodium tablets combined with I 131 in the treatment of patients after thyroidectomy and the effect on thyroglobulin (Tg) and thyroid stimulating hormone (TSH) levels. Methods. 80 patients with differentiated thyroid cancer who required thyroidectomy after surgery between July 2019 and January 2021 were recruited for prospective study, 40 patients in the control group received levothyroxine sodium tablets, and 40 patients in the experimental group received levothyroxine sodium treatment plus I 131 treatment. Treatment effect, serum Tg and TSH levels, and relapse were measured. Results. The removal rate of residual thyroid tissue in the experimental group (87.50%) was significantly higher than that in the control group (57.50%) ( P < 0.05 ). Levothyroxine sodium tablets plus I 131 was associated with a significantly higher efficacy versus levothyroxine sodium tablets ( P < 0.05 ). There were no significant differences in the serum Tg levels between the two groups before treatment ( P > 0.05 ). After treatment, the serum Tg levels in both groups were significantly decreased, and levothyroxine sodium tablets plus I 131 resulted in a significantly lower Tg level versus levothyroxine sodium tablets ( P < 0.05 ). Before treatment, the two groups showed similar TSH levels ( P > 0.05 ). After treatment, patients receiving levothyroxine sodium tablets plus I 131 had a significantly greater increase in the TSH levels versus levothyroxine sodium tablets ( P < 0.05 ). The recurrence rate of the experimental group was lower than that of the control group ( P < 0.05 ). Conclusion. Levothyroxine sodium tablets plus I 131 for post-operative patients with differentiated thyroid cancer enhance the removal rate of residual thyroid tissue, effectively reduce serum Tg level, and increase TSH level, with significant therapeutic effects, low recurrence rates, and a high safety profile.

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“…Co-administration of oral semaglutide with 600 μg of levothyroxine -an oral medication with similar dosing requirements to semaglutide, namely administration once daily on an empty stomach with a full glass of water, 30-60 min before breakfast [24,75] -increased exposure to thyroxine by 33% (AUC 0-48 h,T4 ), supporting the recommendation to avoid coadministration of oral semaglutide within 30 min of other oral medications [24,74]. No obvious effect on thyroxine exposure was seen with SNAC alone, indicating that the increased exposure may be due to the delayed gastric emptying effect of semaglutide [74].…”

Section: Interactions With Drugs Commonly Administered In Patients Wi...mentioning

confidence: 99%

“…Given the mechanism of action of oral semaglutide [56], which includes delayed gastric emptying [24], a number of studies have assessed the impact of oral semaglutide/SNAC on exposure to other commonly administered oral drugs [71][72][73]. In a pharmacokinetic study, co-administration of oral semaglutide with multiple (five) placebo tablets reduced the absorption of semaglutide [74]. Hence, clinical dosing guidance states that other oral medications should be administered at least 30 min after oral semaglutide [24,74].…”

Section: Interactions With Drugs Commonly Administered In Patients Wi...mentioning

confidence: 99%

A new era for oral peptides: SNAC and the development of oral semaglutide for the treatment of type 2 diabetes

Aroda

¹

,

Blonde

²

,

Pratley

³

2022

Rev Endocr Metab Disord

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Glucagon-like peptide-1 (GLP-1) receptor agonists (GLP-1RAs) were first introduced for the treatment of type 2 diabetes (T2D) in 2005. Despite the high efficacy and other benefits of GLP-1RAs, their uptake was initially limited by the fact that they could only be administered by injection. Semaglutide is a human GLP-1 analog that has been shown to significantly improve glycemic control and reduce body weight, in addition to improving cardiovascular outcomes, in patients with T2D. First approved as a once-weekly subcutaneous injection, semaglutide was considered an ideal peptide candidate for oral delivery with a permeation enhancer on account of its low molecular weight, long half-life, and high potency. An oral formulation of semaglutide was therefore developed by co-formulating semaglutide with sodium N-(8-[2-hydroxybenzoyl]amino)caprylate, a well-characterized transcellular permeation enhancer, to produce the first orally administered GLP-1RA. Pharmacokinetic analysis showed that stable steady-state concentrations could be achieved with once-daily dosing owing to the long half-life of oral semaglutide. Upper gastrointestinal disease and renal and hepatic impairment did not affect the pharmacokinetic profile. In the phase III PIONEER clinical trial program, oral semaglutide was shown to reduce glycated hemoglobin and body weight compared with placebo and active comparators in patients with T2D, with no new safety signals reported. Cardiovascular efficacy and safety are currently being assessed in a dedicated outcomes trial. The development of an oral GLP-1RA represents a significant milestone in the management of T2D, providing an additional efficacious treatment option for patients.

show abstract

Effect of oral semaglutide on the pharmacokinetics of thyroxine after dosing of levothyroxine and the influence of co-administered tablets on the pharmacokinetics of oral semaglutide in healthy subjects: an open-label, one-sequence crossover, single-center, multiple-dose, two-part trial

Cited by 15 publications

References 31 publications

Effectiveness and Safety of Levothyroxine Tablets Combined with Iodine-131 in the Treatment of Thyroid Cancer

Effectiveness and Safety of Levothyroxine Tablets Combined with Iodine-131 in the Treatment of Thyroid Cancer

Clinical Efficacy of Levothyroxine Sodium plus I 131 in the Treatment of Patients with Thyroidectomy and Its Effect on the Levels of Thyroglobulin and Thyrotropin

A new era for oral peptides: SNAC and the development of oral semaglutide for the treatment of type 2 diabetes

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