OPKO Health’s OPKO Biologics Doses First Participant in Phase 1/2a Trial of OPK-8801001 for Acromegaly

First-in-human study to evaluate safety, tolerability, pharmacokinetics and pharmacodynamic activity of OPK-8801001, a potential once-weekly, long-acting growth hormone receptor antagonist

KIRYAT GAT, Israel, Oct. 27, 2026 (GLOBE NEWSWIRE) -- OPKO Biologics Ltd., an OPKO Health company (NASDAQ: OPK), today announced that the first participant has been dosed in a first-in-human Phase 1/2a clinical trial of OPK-8801001, an investigational, long acting human growth hormone receptor antagonist being developed for the treatment of acromegaly. The study is designed to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamic activity of OPK-8801001.

OPK-8801001 is being developed using OPKO Biologics’ stabilizer based technology to extend serum half life and reduce injection frequency, with the goal of once weekly administration. In preclinical studies, OPK-8801001 produced robust, dose dependent sustained suppression of insulin-like growth factor-1 (IGF-1), a key marker of disease activity in acromegaly. In vitro studies also demonstrated potent growth hormone receptor antagonism.

“Dosing the first participant marks an important milestone for OPK-8801001 and for OPKO Biologics’ commitment to advancing differentiated therapies for patients with serious endocrine disorders,” said Laura Moschcovich, Ph.D., General Manager of OPKO Biologics. “OPK-8801001 was designed to combine a potent growth hormone receptor antagonist with a long acting stabilizer intended to support less frequent administration. We look forward to evaluating its clinical performance and its potential to improve disease control while reducing treatment burden for people living with acromegaly.”

“The initiation of this first in human study reflects OPKO’s strategy of applying innovative technologies to well-established biological pathways to satisfy persistent meaningful patient needs,” said Phillip Frost, M.D., Chairman and CEO of OPKO Health. “We are pleased to support OPKO Biologics as it advances OPK-8801001 into clinical development and as it continues to build a differentiated endocrinology based pipeline.”

About OPK-8801001
OPK-8801001 is an investigational long-acting hGH receptor antagonist being developed by OPKO Biologics for the treatment of acromegaly. It uses stabilizer-based technology intended to extend serum half life and reduce injection frequency, with the goal of once weekly administration. Preclinical data presented at ENDO 2026 showed robust, dose-dependent and sustained IGF-1 suppression in vivo and approximately 20-fold greater growth hormone receptor antagonism in vitro compared with pegvisomant.

About Acromegaly
Acromegaly is a rare endocrine disorder caused by excess growth hormone, most often due to a benign tumor of the pituitary gland. The condition leads to elevated IGF-1 levels and may be associated with serious complications, including hypertension, diabetes and cardiovascular disease. Despite available therapies, there remains a need for treatment options that provide effective disease control while reducing the burden of ongoing therapy.

About OPKO Biologics
OPKO Biologics is a clinical stage company developing next generation, bio-better, long-acting versions of therapeutic protein and peptide drug candidates using CTP, reversible PEGylation and stabilizer-based technologies. Its pipeline includes candidates for endocrine and gastrointestinal indications, including acromegaly, hypoparathyroidism and short bowel syndrome. OPKO Biologics, an OPKO Health company (NASDAQ: OPK), is based in Kiryat Gat, Israel. For more information, visit www.opkobiologics.com.

About OPKO Health
OPKO Health, Inc. is a multinational biopharmaceutical company focused on developing and delivering therapeutics for serious diseases across global markets. The company’s research and development programs include multispecific antibody technologies, in vivo CAR-T delivered through antibody-guided lipid nanoparticles, and proprietary long-acting peptide and protein engineering capabilities. OPKO also operates specialty pharmaceutical businesses across several international markets. For more information, visit www.opko.com.

Cautionary Statement Regarding Forward-Looking Statements
This press release contains “forward-looking statements,” as that term is defined under the Private Securities Litigation Reform Act of 1995, including, but not limited to, statements regarding the clinical development, safety, tolerability, pharmacokinetics, pharmacodynamic activity, potential efficacy, dosing profile and commercial potential of OPK-8801001. Forward-looking statements are based on current expectations and assumptions and involve risks and uncertainties that could cause actual results to differ materially from those expressed or implied. These risks and uncertainties include, among others, the possibility that clinical development may be delayed or unsuccessful; that results observed in preclinical studies may not be replicated in clinical trials; that regulatory authorities may not approve OPK-8801001; and the risks described in OPKO Health’s filings with the U.S. Securities and Exchange Commission, including its Annual Report on Form 10-K and subsequent reports on Form 10-Q, including, in each case under the headings Risk Factors and Management’s Discussion and Analysis of Financial Condition and Results of Operations. OPKO Health undertakes no obligation to update any forward-looking statement, except as required by law.

Investor and Media Contact
OPKO Health, Inc.
contact@opko.com
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Released October 27, 2026