What data is available regarding equivalent dosing for GLP-1RAs?

Comment by InpharmD Researcher

Equivalent dosing of GLP1-RAs based on a proposed algorithm and recommendations for switching between various GLP-1RAs based on a pharmacokinetic model are presented in Tables 1 and 2, respectively. Switching from an injectable GLP-1RA to an oral agent could be remarkably different from switching between injectable formulations due to patient variability, and additional clinical experiences are still needed to inform appropriate transitions. Overall, conversion between GLP-1RAs is supported by limited high-quality data (see Tables 3-4). Recommendations for transitioning between different GLP-1RAs are primarily based on expert opinion and may not reflect FDA-approved labeling. Generally, details of the current or previous GLP-1RA treatment, glycemic needs, and the presence of gastrointestinal adverse events should be considered to guide initial dosing and titration frequency when switching between agents.

Background

A 2021 review provides guidance for switching from one glucagon-like peptide-1 receptor agonist (GLP-1RA) to another. However, this guidance is also based on the authors’ clinical experience and lacks supporting clinical data. Initially, it is important to consider any contraindications or warnings for the GLP-1RA being switched to that could lead to patient harm. For example, the majority of available GLP-1RAs are not recommended for use in patients with end-stage renal disease. Exceptions to this contraindication are once-weekly semaglutide and dulaglutide. When selecting the dose to initiate, the patient’s history of gastrointestinal (GI) adverse events (AEs) with previous GLP-1RAs should be considered. If there is a history, then it is recommended to switch to a GLP-1RA that allows for slow up-titration, and it should be initiated at the lowest dose, such as 0.25 mg for once-weekly semaglutide and 0.75 mg for dulaglutide. Exenatide extended-release is only available as a single dose and thus cannot be initiated at a lower dose. [1]

When initiating the new GLP-1RA, if the patient has no or minimal GI AEs and/or expresses a preference to initiate at a higher dose, then the authors recommend starting once weekly semaglutide at 0.5 mg, despite incompliant with FDA-approved labeling. Initiating once weekly semaglutide at 1.0 mg is not recommended for the majority of patients due to the increased risk of AEs. The length of time before up-titrating the new GLP-1RA may also be adjusted depending on the presence and/or severity of GI AEs with the initial GLP-1RA. If GI AEs were previously absent/minor, the frequency of up-titration may be increased (e.g., every 2 weeks instead of every 4 weeks), whereas if patients previously experienced substantial GI AEs, waiting longer than 4 weeks before increasing the dose is suggested. [1]

When initiating a new GLP-1RA treatment, details of the current or previous GLP-1RA treatment should also be considered (e.g., how long the patient has been on it, the dose, time of the next dose), which will help guide the dose of the GLP-1RA being switched to. If a lower than maximum dose is being used, the new GLP-1RA should be initiated at the lowest available dose, but if a maximum dose of the initial GLP-1RA is being used, then in the authors’ opinion, initiating at a higher dose can be considered. However, if a patient has only been receiving the initial GLP-1RA for a short duration (<1 month), then the approach to switching to a new GLP-1RA should be the same as the approach taken when initiating that therapy in GLP-1RA naive patients. In patients receiving the initial GLP-1RA for > 1 month, then the dose of the current GLP-1RA should be considered. In general, the first dose of the new GLP-1RA should be given at the time when the next dose of the previous GLP-1RA would have been given. [1]

Doses of concomitant therapies may need adjustment when switching in order to reduce the risk of AEs. For example, in patients who are receiving a sulfonylurea or insulin, the dose may need to be adjusted to reduce the risk of hypoglycemia. An initial 50% dose reduction of sulfonylurea and a 20% reduction of insulin is feasible for most patients based on the authors’ clinical experiences and clinical protocols. In both instances, reductions of doses should be based on baseline HbA1c. All patients should regularly self-monitor blood glucose in the short-term following initiation of the new GLP-1RA to monitor for hypoglycemia and inform any decisions concerning subsequent dose changes. Additionally, dipeptidyl peptidase-4 inhibitors should be discontinued when initiating GLP-1RAs, as the mechanism of action of these two drug classes is not synergistic. [1]

Once a patient is initiated on a new GLP-1RA, they should be monitored for GI AEs with subsequent dose up-titrations to achieve greater effectiveness if needed. In the absence of GI AEs, the authors believe up-titration may be performed rapidly (i.e., increasing to the next dose after 2-4 weeks), regardless of recommendations from prescribing information. If GI AEs are present, a more cautious approach with slower-up titration (i.e., every 4 to 8 weeks) should be taken. If GI AEs are intolerable to the patient after several weeks following up-titration, the patient could be moved back to a lower dose. Antiemetics may be prescribed for short periods if GI AEs are severe and the patient wishes to remain on a GLP-1RA. However, if GI AEs have not reduced after a course of antiemetics is complete, the patient may need to be switched from the GLP-1RA to an alternative glucose-lowering therapy. [1]

A 2020 review proposed a practical algorithm for switching between once-daily and once-weekly GLP-1RA therapies, but the algorithm is primarily based on the authors’ clinical experience and is not supported by clinical data. When the decision to switch GLP-1RAs is made, the current GLP-1RA should be discontinued, and the patient should be counseled on the differences between the two agents. It is suggested that patients can generally be switched from once daily, twice daily, or once weekly GLP-1RAs to any other GLP-1RA (i.e., once daily, twice daily, or once weekly). If a patient is being switched from a once daily or twice daily GLP-1RA, the first dose of the new GLP-1RA should be administered the following day after discontinuation. In cases when patients are switching from a once-weekly GLP-1RA, the first dose of the new GLP-1RA should be administered 7 days after discontinuation. [2]

When initiating the switch, the new agent should be initiated after waiting for symptoms to resolve if the switch was prompted by GI side effects. The new agent is recommended to be started at the lowest available dose, and slower titration to the maximum dose should be considered. A lower maintenance dose can be considered if needed due to GI AEs. If the switch was prompted by other reasons and not GI intolerance, it is the opinion of the authors that the new agent should be started with an equivalent (or lower) dose (see Table 1) and titrated according to prescribing information. The assessment of equivalent dose is noted to be entirely based on the authors’ opinion, which is said to be based on head-to-head clinical trials when available and/or clinical experience. The patient should be re-evaluated every 2 to 3 months for side effects, adequate titration, and glycemic response. Authors noted that switching from injectable GLP-1RA to an oral agent could be remarkably different from switching between injectable formulations, and additional clinical experiences are still needed to inform appropriate transition. [2]

A 2022 Saudi guideline provides a consensus for switching between GLP-1 RAs based on available randomized controlled trials and two review articles. The guideline recommends an individualized approach and several considerations such as adverse effects with the current GLP-1RA, duration of current GLP-1RA therapy, glycemic control needed, and patients’ preferences. A summary of changes in HbA1c and weight reduction observed in clinical studies after switching GLP-1RAs can be found in Table 3. [3]

A 2018 study utilizing a pharmacokinetic simulation model and observational data from four phase 3 semaglutide trials evaluated the impact of switching treatment from another GLP-1RA to semaglutide. A 26-week simulated treatment with liraglutide 1.2 or 1.8 mg, dulaglutide 0.75 or 1.5 mg, or exenatide extended-release 2.0 mg was followed by a simulated semaglutide treatment 1 day after the last once-daily dose of liraglutide and 1 week after the last once-weekly doses of dulaglutide or exenatide extended-release. The dose of semaglutide was gradually increased from 0.25 mg to 0.5 mg and eventually to 1 mg. At week 52, decreases in HbA1c ranged from ~0.3% to ~0.8%-points and reduction in body weight from ~2% to ~4% with semiglutide 1.0 mg. A summary of effects on HbA1c during the transition from other GLP-1RA to semaglutide 0.25 or 0.5 mg is presented in Table 2. Of note, this exposure-response modeling only reflects mean outcomes and is not adjusted for variations among individual patients. Additionally, other clinical outcomes besides weight loss cannot be extrapolated from the study findings. [4]

References:

[1] Jain AB, Ali A, Gorgojo Martínez JJ, et al. Switching between GLP-1 receptor agonists in clinical practice: Expert consensus and practical guidance. Int J Clin Pract. 2021;75(2):e13731. doi:10.1111/ijcp.13731
[2] Almandoz JP, Lingvay I, Morales J, Campos C. Switching Between Glucagon-Like Peptide-1 Receptor Agonists: Rationale and Practical Guidance. Clin Diabetes. 2020;38(4):390-402. doi:10.2337/cd19-0100
[3] Alsifri, S., Elbadawi, H., Alsabaan, F. et al. Saudi consensus for GLP-1 RAs switching guidance: consensus report. International Journal of Clinical Medicine.2022;13 (1): 22-35.
[4] Overgaard RV, Lindberg SØ, Thielke D. Impact on HbA1c and body weight of switching from other GLP-1 receptor agonists to semaglutide: A model-based approach. Diabetes Obes Metab. 2019;21(1):43-51. doi:10.1111/dom.13479


Literature Review

A search of the published medical literature revealed 4 studies investigating the researchable question:

What data is available regarding equivalent dosing for GLP-1RAs?

Level of evidence

D - Case reports or unreliable data  Read more→



Please see Tables 1-4 for your response.


Equivalent Doses of GLP-1 Receptor Agonists
Agent Frequency Equivalent Dose
Exenatide Once weekly - - 2 mg -
Dulaglutide Once weekly - 0.75 mg 1.5 mg -
Semaglutide Once weekly - 0.25 mg 0.5 mg 1 mg
Liraglutide Once daily 0.6 mg 1.2 mg 1.8 mg -
Lixisenatide Once daily 10 mcg 20 mcg - -
Oral semaglutide Once daily 3 mg 7 mg 14 mg -
Exenatide Twice daily 5 mcg 10 mcg - -
References:

Adapted from:
Almandoz JP, Lingvay I, Morales J, Campos C. Switching Between Glucagon-Like Peptide-1 Receptor Agonists: Rationale and Practical Guidance. Clin Diabetes. 2020;38(4):390-402. doi:10.2337/cd19-0100

Summary of the effects on HbA1c during transition after switching from another GLP-1RA to semaglutide at a starting dose of 0.25 or 0.5 mg

Initial treatment Switch to semaglutide 0.25 mg Switch to semaglutide 0.5 mga
Liraglutide 1.2 mg Small transient HbA1c increase Stable HbA1c
Liraglutide 1.8 mg Small transient HbA1c increase Stable HbA1c
Dulaglutide 0.75 mgb Stable HbA1c Immediate improvementin HbA1c
Dulaglutide 1.5 mg Small transient HbA1c increase Stable HbA1c
Exenatide ER 2.0 mgc Gradual improvement in HbA1c Immediate improvement in HbA1c

Abbreviations: ER, extended-release; GLP-1RA, glucagon-like peptide-1receptor agonist; HbA1c, glycated hemoglobin.
aIt should be noted that semaglutide is currently marketed at a starting dose of 0.25 mg.
bCautious initiation of semaglutide is recommended because of low effect compared to semaglutide 0.5 mg.
cCautious initiation of semaglutide is recommended as exenatide ER pharmacokinetics are extended beyond 1 week.

References:

Adapted from:
Overgaard RV, Lindberg SØ, Thielke D. Impact on HbA1c and body weight of switching from other GLP-1 receptor agonists to semaglutide: A model-based approach. Diabetes Obes Metab. 2019;21(1):43-51. doi:10.1111/dom.13479

Summary of HbA1c and weight reduction after switching to another GLP-1RA1
Study From To Effect
DURATION 1 trial2 Exenatide 10 mcg twice daily  Exenatide ER 2.0 mg daily

Further HbA1c reduction: 0.2%

LEAD 6 trial3 Exenatide 10 mcg twice daily  Liraglutide 1.8 mg daily

Further HbA1c reduction: 0.3%

Further weight reduction: 0.9 kg

CIBELES Project4

Exenatide 5 to 10 mcg twice daily 

Liraglutide 1.2 to 1.8 mg daily

Lixisenatide 20 mcg daily

Dulaglutide 1.5 mg weekly

Exenatide once weekly* Further HbA1c reduction: 0.4%
Visaria et al.5 Another GLP-1RA* Semaglutide once weekly* Further HbA1c reduction: 1.3%
REALiSe-DM trial6

Liraglutide once daily*

Dulaglutide once weekly*

Semaglutide once weekly*

Further HbA1c reduction: 0.7%

Mean reduction in weight: 1.6 kg

Watanabe et al.7

Exenatide 10 to 20 mcg twice daily

Exenatide ER once weekly*

Further HbA1c reduction: 0.2% 

Reduction in the incidence of hypoglycemia 

 Goncalves and Bell8 Liraglutide 1.8 mg daily Semaglutide once weekly (average dose: 0.76 mg)

Further HbA1c reduction: decreased from 7.46% ± 1.36% to 6.68% ± 1.00%

Weight reduction: dropped from 110.6 ± 20 kg to 106 ± 27 kg.

Insulin requirement: number of patients requiring insulin dropped from 16 to 13

Overgaard et al. modeling9

Liraglutide 1.2 to 1.8 mg daily

Dulaglutide 0.75 mg to 1.5 mg weekly

Exenatide ER 2.0 mg weekly

Semaglutide 0.25 to 0.5 mg once weekly Further HbA1c and weight reduction were observed

ER, extended-release; GLP-1RA, glucagon-like peptide-1receptor agonist; HbA1c, glycated hemoglobin

*Doses of the GLP-1RA used were not provided in the published article.

References:

[1] Alsifri, S., Elbadawi, H., Alsabaan, F. et al. Saudi consensus for GLP-1 RAs switching guidance: consensus report. International Journal of Clinical Medicine.2022;13 (1): 22-35.
[2] ​​​​Buse JB, Drucker DJ, Taylor KL, et al. DURATION-1: exenatide once weekly produces sustained glycemic control and weight loss over 52 weeks. Diabetes Care. 2010;33(6):1255-1261. doi:10.2337/dc09-1914.
[3] Buse JB, Sesti G, Schmidt WE, et al. Switching to once-daily liraglutide from twice-daily exenatide further improves glycemic control in patients with type 2 diabetes using oral agents. Diabetes Care. 2010;33(6):1300-1303. doi:10.2337/dc09-2260
[4] Gorgojo-Martínez JJ, Gargallo-Fernández MA, Brito-Sanfiel M, Lisbona-Catalán A. Real-world clinical outcomes and predictors of glycaemic and weight response to exenatide once weekly in patients with type 2 diabetes: The CIBELES project. Int J Clin Pract. 2018;72(3):e13055. doi:10.1111/ijcp.13055
​​​​[5] Visaria, J., Dang-Tan, T., Petraro, P.V., Nepal, B.K. and Willey, V., 2019. 1006-P: real-world effectiveness of semaglutide in early users from a US commercially insured (CI) and medicare advantage (MA) population. Diabetes, 68(Supplement_1).
[6] Jain AB, Kanters S, Khurana R, Kissock J, Severin N, Stafford SG. Real-World Effectiveness Analysis of Switching From Liraglutide or Dulaglutide to Semaglutide in Patients With Type 2 Diabetes Mellitus: The Retrospective REALISE-DM Study. Diabetes Ther. 2021;12(2):527-536. doi:10.1007/s13300-020-00984-x
[7] ​​Watanabe Y, Saisho Y, Inaishi J, et al. Efficacy and safety of once-weekly exenatide after switching from twice-daily exenatide in patients with type 2 diabetes. J Diabetes Investig. 2020;11(2):382-388. doi:10.1111/jdi.13146
[8] Goncalves E, Bell DS. Efficacy of semaglutide versus liraglutide in clinical practice. Diabetes Metab. 2020;46(6):515-517. doi:10.1016/j.diabet.2019.10.001
[9] Overgaard RV, Lindberg SØ, Thielke D. Impact on HbA1c and body weight of switching from other GLP-1 receptor agonists to semaglutide: A model-based approach. Diabetes Obes Metab. 2019;21(1):43-51. doi:10.1111/dom.13479

 

Switch-to-Semaglutide Study (STS-Study): a Retrospective Cohort Study

Design

Retrospective cohort study

N= 77

Objective

To systematically investigate the efficacy of glucose control and weight change over 6 months of a switch to semaglutide from any other GLP-1 analog therapy in a real-world clinical practice setting

Study Groups

Equipotent switch (n= 61)

Stepwise switch (n= 16)

Inclusion Criteria

Type 2 diabetes, age 18 years or older, use of GLP-1 analog for 3 months or longer

Exclusion Criteria

Other types of diabetes, significant glucose-altering medication (e.g., glucocorticosteroids or other diabetes medication) was initiated concomitantly with semaglutide

Methods

Patient data that fulfilled the criteria were included for analysis. GLP-1 analogs may have included either liraglutide, dulaglutide, exenatide, or oral semaglutide. Patients may also have been receiving concomitant diabetes or insulin therapy so long as it was not initiated at the start of semaglutide switch. The comparator consisted of HbA1c levels 3 to 6 months prior to switching to semaglutide.

Some patients may have undergone an equipotent dosing switch based on a theoretical model, which has yet to be vetted clinically [2]. The model assumes that patients were on 26-week stable regimens of liraglutide 1.2 mg, liraglutide 1.8 mg, dulaglutide 0.75 mg, dulaglutide 1.5 mg, or exenatide ER 2.0 mg. Semaglutide is to be initiated 1 day after liraglutide and 1 week after dulaglutide or exenatide ER at either 0.25 mg or 0.5 mg. The model suggests that some switches may achieve stable HbA1c starting with higher doses of semaglutide, but this study did not adequately describe the method of equipotent dose switching.

Other patients underwent a stepwise dosing approach starting at 0.25 mg subcutaneously (SubQ) once weekly. The max recommended dose is semaglutide 1 mg per week.

Duration

Data collection period: January 1, 2018, to December 31, 2019

Outcome Measures

Subgroup analysis of change in HbA1c and weight, kg at 3 and 6 months after switching to semagluide

Baseline Characteristics

 

Study participants (N= 77)

     

Age, years

61      

Female

27 (35%)       

Weight, kg

101      

Body mass index, kg/m2

35      

Preceding GLP-1 analogue

Liraglutide

Dulaglutide

Exenatide

Orally-administered semaglutide

 

61 (79.2%)

11 (14.0%)

3 (3.8%)

2 (2.6%)

     

Concomitant oral diabetes

Metformin

Pioglitazone

Sulfonylurea

SGLT2 inhibitor

 

61 (79%)

4 (5.2%)

16 (20.7%)

8 (10.3%)

     

Concomitant insulin therapy

Basal insulin

Prandial insulin

 

56 (72.7%)

12 (15.5%)

     

Results

Endpoint

Equipotent switch (n= 61)

p-value versus baseline

Stepwise switch (n= 16)

p-value versus baseline

Absolute HbA1c levels

3-6 month pre-baseline

Baseline

3-month post-switch

6-month post-switch

 

8.2%

8.3%

7.6%

7.3%

 

--

--

< 0.0001

< 0.0001

 

8.8%

9.0%

8.0%

8.2%

 

--

--

< 0.005

Not significant

Mean weight, kg

Baseline

3-month post-switch

6-month post-switch

 

102

101

99

 

--

< 0.0001

< 0.0001

 

96

94

93

 

--

0.6592

0.0690

Adverse Events

All events were reported in the equipotent switch group. Most common events were nausea (6.4%), vomiting (5.2%), and diarrhea (6.4%). Two patients were hospitalized due to gastrointestinal symptoms. Three patients were discontinued due to side effects.

Study Author Conclusions

Switching to semaglutide from established GLP-1 analog therapy improved HbA1c and body weight. Both equipotential and stepwise dosing initiation appear to be effective and well tolerated.

InpharmD Researcher Critique

The exact dose between the equipotent switching from other GLP-1 analogs to subcutaneous semaglutide was not described within the study. Instead, a theoretical model was referenced that observed liraglutide, dulaglutide, and exenatide. Without clear instructions, the optimal switching to semaglutide cannot be verified.



References:

[1] Hepprich M, Zillig D, Florian-Reynoso MA, Donath MY, Rudofsky G. Switch-to-Semaglutide Study (STS-Study): a Retrospective Cohort Study. Diabetes Ther. 2021;12(3):943-954. doi:10.1007/s13300-021-01016-y
[2] Overgaard RV, Lindberg SØ, Thielke D. Impact on HbA1c and body weight of switching from other GLP-1 receptor agonists to semaglutide: A model-based approach. Diabetes Obes Metab. 2019 Jan;21(1):43-51. doi: 10.1111/dom.13479. Epub 2018 Aug 23. PMID: 30047216; PMCID: PMC6585654.