Delving into the Latest Updates on Ersodetug with Synapse

RegulationBreakthrough Therapy (United States), Orphan Drug (United States), Orphan Drug (European Union), PRIME (European Union), Rare Pediatric Disease (United States)

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Structure/Sequence

Sequence Code 719971371L

Source: *****

Sequence Code 719971495H

Source: *****

The Phase 3 pivotal study is designed to evaluate the efficacy and safety of RZ358 for the treatment of congenital hyperinsulinism (HI) as add-on to standard-of-care (SOC) therapy compared to SOC alone over 24 weeks and to evaluate the longer-term safety and efficacy of RZ358 during a subsequent open-label extension (OLE) period.

Start Date11 Jan 2024

Sponsor / Collaborator

Rezolute, Inc.

NCT04538989

/ CompletedPhase 2

An Open-Label Multiple-Dose Study of RZ358 in Patients With Congenital Hyperinsulinism

The objective of this trial is to evaluate the safety, tolerability and glucose-raising effects of RZ358 in patients with Congenital Hyperinsulinism (HI).

Start Date24 Feb 2020

Sponsor / Collaborator

Rezolute, Inc.

100 Clinical Results associated with Ersodetug

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100 Translational Medicine associated with Ersodetug

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100 Patents (Medical) associated with Ersodetug

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2

Literatures (Medical) associated with Ersodetug

01 Jun 2025·Med

Global, multi-center, repeat-dose, phase 2 study of RZ358 (ersodetug), an insulin receptor antibody, for congenital hyperinsulinism

Article

Author: Melikyan, Maria ; Roberts, Brian K ; Demirbilek, Huseyin ; Mohnike, Klaus ; Galcheva, Sonya ; O'Boyle, Erin ; Dastamani, Antonia ; Christesen, Henrik Thybo ; Kheladze, Nino ; Thornton, Paul S ; Empting, Susann ; Iotova, Violeta ; Clemente, Maria ; De Leon, Diva D ; Mazor-Aronovitch, Kineret ; Hood, Davelyn ; Ozbek, Mehmet Nuri

BACKGROUND:

Congenital hyperinsulinism (cHI) is a rare, primarily pediatric disease characterized by dysregulated insulin secretion resulting in severe, persistent hypoglycemia, frequently leading to lifelong neurologic impairments. The safety, pharmacokinetics, and glycemic efficacy of ersodetug, a fully human monoclonal antibody that allosterically and reversibly binds the insulin receptor (INSR) and reduces excess insulin action, are being evaluated for the treatment of cHI-related hypoglycemia.

METHODS:

A global, open-label, phase 2b study (ClinicalTrials.gov: NCT04538989) was conducted in 23 patients with cHI with persistent hypoglycemia on standard-of-care (SOC) therapies. Eligible participants (age ≥2 years) received add-on ersodetug at dose levels between 3 and 9 mg/kg intravenously (i.v.) bi-weekly for 8 weeks in 4 sequential dose cohorts.

FINDINGS:

Enrolled participants (average age = 6.7 years) on SOC (87% medications; 17% previous pancreatectomy) experienced 13 events/week and 23% time in hypoglycemia at baseline. Ersodetug resulted in predictable, dose-proportional pharmacokinetics. No deaths, adverse drug reactions, study withdrawals, or dose-limiting toxicities occurred. Hypoglycemia (<70 mg/dL) events (self-monitored blood glucose) and time (continuous glucose monitoring) improved from baseline by medians of 59% (p < 0.001) and 54% (p < 0.001), respectively, across pooled dose levels and by 48%-84% (events) and 61%-65% (time) at doses of 6 or 9 mg/kg (p < 0.05) with a nearly universal individual patient response rate. Additional hypoglycemia metrics, including overnight hypoglycemia, similarly improved.

CONCLUSION:

Ersodetug was generally well tolerated and significantly improved hypoglycemia in participants with cHI. Ersodetug represents a novel INSR-targeted mechanism of action with the potential to be an effective therapy for all forms of cHI, alone or in combination with other therapies.

FUNDING:

Rezolute, Inc. (Redwood City, CA), provided funds.

01 Aug 2017·The Journal of clinical endocrinology and metabolismQ2 · MEDICINE

Attenuation of Insulin Action by an Allosteric Insulin Receptor Antibody in Healthy Volunteers

Q2 · MEDICINE

Article

Author: Ann Neale ; Allan Gordon ; Kirk W Johnson ; Padma Bezwada ; Sabine Vukelich ; Paul Rubin ; Ira Goldfine ; Julie Roessig

Background:

XOMA 358 (X358) is a fully human monoclonal antibody to the insulin receptor that acts as a negative allosteric modulator of insulin signaling. It is being developed as a novel treatment of hyperinsulinemic hypoglycemia. This report describes pharmacokinetic (PK) and pharmacodynamic (PD) data from a first-in-human clinical trial.

Methods:

A double-blind, placebo-controlled, single-ascending-dose study was performed with 29 healthy adult males randomized to intravenous infusion of placebo or X358 at 0.1-, 0.3-, 1-, 3-, 6-, or 9-mg/kg dose levels. The primary objective was to assess safety and tolerability, and secondary objectives included PK and PD analyses. A short insulin tolerance test (ITT) was implemented in the 3- to 9-mg/kg dose cohorts at baseline and postinfusion.

Results:

There were no deaths, serious adverse events (AEs), or subject discontinuations due to AEs. There were no clinically meaningful safety findings. X358 exhibited dose-proportional PK with a half-life of 21 days. Dose-dependent elevations of circulating insulin levels, likely related to reduced insulin clearance via monoclonal antibody action at receptors, represented a sensitive biomarker of X358 exposure. X358-dependent increases in postprandial glucose levels and fasting homeostatic model assessment of insulin resistance values were observed and persisted for at least 1 week at the higher dose levels. In all the ITT cohorts, the slope for glucose lowering was substantially attenuated after X358 infusion of a similar magnitude, but with increasing duration with rising dose level.

Conclusion:

Single X358 infusions were well tolerated and resulted in a dose-dependent reduction in insulin sensitivity. Clinical development of X358 in hyperinsulinemic, hypoglycemic conditions is proceeding.

104

News (Medical) associated with Ersodetug

02 Sep 2026

·www.globenewswire.com

Rezolute to Participate in Upcoming Investor Conferences

REDWOOD CITY, Calif., Sept. 02, 2026 (GLOBE NEWSWIRE) -- Rezolute, Inc. (Nasdaq: RZLT) (“Rezolute” or the “Company”), a late-stage ultra-rare disease company focused on treating refractory hypoglycemia caused by a congenital or any acquired form of hyperinsulinism (HI), today announced that management will participate in the following investor conferences: Event: Cantor Global Healthcare ConferenceDate: September 9-11, 2026 Event: H.C. Wainwright 28th Annual Global Investment Conference Date: September 14-16, 2026 Event: Morgan Stanley 24th Annual Global Healthcare ConferenceDate: September 14-16, 2026 Management will be participating in fireside chats and one-on-one investor meetings throughout the conferences. Investors interested in scheduling a meeting with the Rezolute management team should contact their Cantor, H.C. Wainwright, and Morgan Stanley representatives. About Rezolute, Inc. Rezolute is a late-stage ultra-rare disease company focused on treating refractory hypoglycemia caused by a congenital or any acquired form of hyperinsulinism (HI). The Company’s antibody therapy, ersodetug, has been studied in clinical trials and used in real-world cases for the treatment of refractory hypoglycemia due to a variety of causes of HI. For more information, visit www.rezolutebio.com. Rezolute Contacts: Christen Baglaneascbaglaneas@rezolutebio.com508-272-6717 Carrie McKimcmckim@rezolutebio.com 336-608-9706

02 Sep 2026

·www.biospace.com

Rezolute to Participate in Upcoming September 2026 Investor Conferences

REDWOOD CITY, Calif., Sept. 02, 2026 (GLOBE NEWSWIRE) -- Rezolute, Inc. (Nasdaq: RZLT) (“Rezolute” or the “Company”), a late-stage ultra-rare disease company focused on treating refractory hypoglycemia caused by a congenital or any acquired form of hyperinsulinism (HI), today announced that management will participate in the following investor conferences: Event : Cantor Global Healthcare Conference Date : September 9-11, 2026 Event : H.C. Wainwright 28 th Annual Global Investment Conference Date : September 14-16, 2026 Event : Morgan Stanley 24 th Annual Global Healthcare Conference Date : September 14-16, 2026 ezstandalone.cmd.push(function () { ezstandalone.showAds(131); }); Management will be participating in fireside chats and one-on-one investor meetings throughout the conferences. Investors interested in scheduling a meeting with the Rezolute management team should contact their Cantor, H.C. Wainwright, and Morgan Stanley representatives. About Rezolute, Inc. Rezolute is a late-stage ultra-rare disease company focused on treating refractory hypoglycemia caused by a congenital or any acquired form of hyperinsulinism (HI). The Company’s antibody therapy, ersodetug, has been studied in clinical trials and used in real-world cases for the treatment of refractory hypoglycemia due to a variety of causes of HI. For more information, visit . Rezolute Contacts: ezstandalone.cmd.push(function () { ezstandalone.showAds(132); }); Christen Baglaneas cbaglaneas@rezolutebio.com 508-272-6717 Carrie McKim cmckim@rezolutebio.com 336-608-9706

21 Jul 2026

·www.globenewswire.com

Rezolute to Participate in the BTIG Virtual Biotechnology Conference

REDWOOD CITY, Calif., July 21, 2026 (GLOBE NEWSWIRE) -- Rezolute, Inc. (Nasdaq: RZLT) (“Rezolute” or the “Company”), a late-stage ultra-rare disease company focused on treating refractory hypoglycemia caused by a congenital or any acquired form of hyperinsulinism (HI), today announced that management will participate in the BTIG Virtual Biotechnology Conference, taking place July 28-29, 2026. Management will be participating in one-on-one investor meetings throughout the conference. Investors interested in scheduling a meeting with the Rezolute management team should contact their BTIG representative. About Rezolute, Inc. Rezolute is a late-stage ultra-rare disease company focused on treating refractory hypoglycemia caused by a congenital or any acquired form of hyperinsulinism (HI). The Company’s antibody therapy, ersodetug, has been studied in clinical trials and used in real-world cases for the treatment of refractory hypoglycemia due to a variety of causes of HI. For more information, visit www.rezolutebio.com. Rezolute Contacts: Christen Baglaneascbaglaneas@rezolutebio.com508-272-6717 Carrie McKimcmckim@rezolutebio.com 336-608-9706

100 Deals associated with Ersodetug

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External Link

KEGG	Wiki	ATC	Drug Bank
D12912	-	-	-

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Hyperinsulinism	Phase 3	Netherlands	Rezolute, Inc.	16 Apr 2025
Hyperinsulinism	Phase 3	Switzerland	Rezolute, Inc.	16 Apr 2025
Hypoglycemia	Phase 3	Netherlands	Rezolute, Inc.	16 Apr 2025
Hypoglycemia	Phase 3	Switzerland	Rezolute, Inc.	16 Apr 2025
Ichthyosis, Lamellar	Phase 3	United States	Rezolute, Inc.	16 Apr 2025
Ichthyosis, Lamellar	Phase 3	France	Rezolute, Inc.	16 Apr 2025
Ichthyosis, Lamellar	Phase 3	Netherlands	Rezolute, Inc.	16 Apr 2025
Ichthyosis, Lamellar	Phase 3	Switzerland	Rezolute, Inc.	16 Apr 2025
Ichthyosis, Lamellar	Phase 3	United Kingdom	Rezolute, Inc.	16 Apr 2025
Congenital Hyperinsulinism	Phase 3	-	Rezolute, Inc.	14 Dec 2023

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT06208215 (sunRIZE, GlobeNewswire) Manual	Phase 3	Congenital Hyperinsulinism	-	Ersodetug 5 mg/kg	zgrrpxdafd(hzselzwgre) = xvqwbanudm asnjpbcyqz (fxchjoawfj ) Not Met	Negative	11 Dec 2025
				Ersodetug 10 mg/kg	zgrrpxdafd(hzselzwgre) = wigwormjvq asnjpbcyqz (fxchjoawfj ) Not Met View more
NCT04538989 (Global, multi-center, repeat-dose, phase 2 study of RZ358, Pubmed \| Med)	Phase 2	Congenital Hyperinsulinism Add-on	23	Ersodetug 3 mg/kg	ygapiszndd(boxtpmqknu) = kxansujaoc ectxgdezjl (vnkqgrqtsi ) View more	Positive	01 Jun 2025
				Ersodetug 6 mg/kg	ygapiszndd(boxtpmqknu) = lijelfpnrq ectxgdezjl (vnkqgrqtsi ) View more
NCT04538989 (Global, multi-center, repeat-dose, phase 2 study of RZ358 \| RIZE, CTgov)	Phase 2	Congenital Hyperinsulinism	23	RZ358 Sequential Group Cohort 1 (RZ358 Cohort 1)	uwlbbwkptw(oekrhqrzns) = ifqzrjqvki stycomiblj (zgmxpllduz, fmxogccfmd - ywtqidnmrz) View more	-	28 May 2025
				RZ358 Sequential Group Cohort 2 (RZ358 Cohort 2)	uwlbbwkptw(oekrhqrzns) = yljuogiofw stycomiblj (zgmxpllduz, qrluzgcoky - qhkfepwupm) View more
NCT04538989 (RIZE, ESPE2022)	Phase 2	Congenital Hyperinsulinism	23	RZ358 3mg/kg	esqokilier(nwljupohjs) = famurcicbr mdqcukbmpx (wcesogyuxj )	Positive	15 Sep 2022
				RZ358 6mg/kg	esqokilier(nwljupohjs) = xxthnwzsst mdqcukbmpx (wcesogyuxj )
NCT04538989 (RIZE, Corporate Publications) Manual	Phase 2	Congenital Hyperinsulinism	22	RZ358	wrvdqhpxvc(rnazajvgyu) = ywokuyyxjs cjxsuggmln (thgrbcgpec ) View more	Positive	01 May 2022
ENDO2021	Phase 2	Hypoglycemia insulin \| c-peptide \| ketones ... View more	16	RZ358 3 mg/kg	qweapmgbpl(uxhsdjejin) = concentration-dependent increases bvilblbapt (clpanjdqqm ) View more	Positive	03 May 2021
				RZ358 6 mg/kg

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Ersodetug

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