Drug name
Last update: Aug 2026Insulin efsitora
Developer(s)
Drug information
Insulin efsitora (LY3209590) (basal insulin Fc)
Not provided
Biotherapeutic
Not provided
Insulin efisitora alfa is a long-acting fusion protein administered once weekly for the management of type 2 diabetes mellitus. It exhibits a terminal half-life (t₁/₂) of approximately 17 days, supporting a sustained and dose-dependent reduction in fasting blood glucose levels for five days or longer. The maximum observed plasma concentration (C_max) is approximately 30 nmol/L. Clinical trial data suggest that insulin efisitora alfa has a favorable safety profile, with no reports of severe hypoglycemia. However, at a 10 mg dose, 83% of patients experienced at least one adverse event.
Not yet approved
Not yet approved
Therapeutic area(s)
- Diabetes
- Treatment
Administration route
Subcutaneous
Associated long-acting platforms
Solution
Use of drug
- Administered by a nurse
- Self-administered
- Administered by a community health worker
- Administered by a specialty health worker
- Weekly
Dosage
500 units/mL
Not provided
Dosage Regimen for Efsitora (500 units/mL): 1. Loading Dose (Week 1—First Injection Only): Administer a one-time loading dose calculated as usual daily basal insulin dose (units) × 7 (rounded to the nearest 10 units) × 3. This loading dose is intended to provide weekly basal coverage. 2. Maintenance Dose (Week 2 Onwards): Administer a weekly dose calculated as usual daily basal insulin dose (units) × 7 (rounded to the nearest 10 units) × 3. This dose should be given once weekly thereafter.
Not provided
Not provided
Associated compounds, formulations and regimens
Not provided
Associated technologies
Not provided
Additional information
Developer(s)
Eli Lilly
Eli Lilly and Company, commonly known as Lilly, is an American multinational pharmaceutical company headquartered in Indianapolis, Indiana. Founded nearly 150 years ago, Lilly focuses on developing medicines that improve lives worldwide. The company is renowned for its contributions in biomedicine and pharmaceuticals, with a diverse portfolio including well-known products like Trulicity, Jardiance
Drug structure
Scale-up and manufacturing prospects
Not provided
1. Bioreactor 2. Seed culture tanks 3. Homogenizer 4. Reaction vessel 5. Stirrer 6. Inert gas supply systems 7. Ultrafiltration units
1. Recombinant Expression of Insulin in Saccharomyces cerevisiae 2. Purification of insulin analog 3. Site-specific conjugation 4. Purification of the conjugated insulin 5. Excipient addition and formulation preparation
1. Ion-exchange chromatography/Reverse-phase chromatography/Size-exclusion chromatography 2. High-Performance Liquid Chromatography (HPLC)
Excipients & delivery device(s)
No proprietary excipient used
No novel excipient or existing excipient used
No residual solvent used
Not provided
Safety, Efficacy and Evidence Summary
Not provided
Not provided
Not provided
Not provided
Efsitora alfa formulations
Described herein are preserved formulations of insulin-Fc fusions. The formulations include insulin-Fc fusions having prolonged pharmacokinetic and pharmacodynamic profiles sufficient for once weekly administration in the treatment of diabetes and are sufficiently stable to allow for storage and use without unacceptable loss of chemical or physical stability.
WO2023086980
Formulation
ELI LILLY AND COMPANY
Not provided
November 14, 2042
Pending: AE, DZ, AR, ARIPO, AU, BH, BR, BN, CA, CL, CN, CO, CR, DO, EC, EG, EAPO, EPC, GT, HN, HK, ID, IL, JP, JO, KR, KW, LB, LK, MO, MY, MX, NZ, NG, OM, PK, PA, PE, PH, QA, SA, SG, SV, TW, TH, TT, UA, US, VE, VN , ZA
Insulin Efsitora Alfa Method of Treatment Diabetes
Described herein are doses and dosing regimens comprising determining and administering doses of long-acting insulin receptor agonists suitable for once-weekly dosing, such as Weekly Basal Insulin-Fc (BIF).
WO2022132709
Method of Treatment
ELI LILLY AND COMPANY
Not provided
December 14, 2041
Granted: AU, EAPO Pending: BR, CA, CN, EAPO, EPC, KR, JP, IL, MX, NZ, SG, TH, US
Insulin Efsitora Alfa Method of Treatment Diabetes
Described herein are fixed doses and dosing regimens for long-acting insulin receptor agonists suitable for once-weekly dosing, such as weekly basal insulin-Fc (BIF).
WO2022132712
Method of Treatment
ELI LILLY AND COMPANY
Not provided
December 14, 2041
Granted: AU, EAPO Pending: BR, CA, CN, EAPO, EPC, KR, JP, IL, MX, NZ, SG, TH, US
Efsitora alfa compound and analogues
The present invention relates to fusion proteins comprising an insulin receptor agonist fused to a human IgG Fc region through the use of a peptide linker, and the use of such fusion proteins in the treatment of diabetes. The fusion protein of the present invention has an extended time action profile and is useful for providing basal glucose control for an extended period of time.
WO2016178905
compound
ELI LILLY AND COMPANY
Not provided
April 28, 2025
Granted: ARIPO (BW, GH, KE, NA), AU, BR, CL, CN, DZ, CO, EA (RU), EP (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LI, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, TR, BA, ME, MA, MD), IN, JP, JO, KR, LB, MX, NZ, NG, PE, PH, PK, SG, LK, TW, UA, US, ZA Pending: AR, BN, CA, DO, EC, EG, SV, GT, GC, HN, HK, ID, IL, MO, MY, PA, TH, TT, TN, VE, VN