Safety, Tolerability, and Pharmacokinetics of EGT710, a Novel Coronavirus Mpro Inhibitor, in Healthy Adults: A Randomized, Single- and Multiple-Dose Study.
9 affiliations
- 1ICON Plc, Groningen, The Netherlands.
- 2CA CSI CVM, Biomedical Research, Novartis, Cambridge, MA, USA.
- 3Global Health, Research & Development, Pharmacokinetics, Novartis Pharma AG, Basel, Switzerland.
- 4Early Development Analytics, Development, Novartis Pharmaceuticals Corporation, Cambridge, MA, USA.
- 5Preclinical Safety, Biomedical Research, Novartis Pharma AG, Basel, Switzerland.
- 6Preclinical Safety, Novartis Pharmaceuticals Corporation, East Hanover, NJ, USA.
- 7CS&I Immunology, Biomedical Research, Novartis Pharma AG, Basel, Switzerland.
- 8Biostatistics & Pharmacometrics, Novartis Healthcare Private Limited, Mumbai, India.
- 9Translational Medicine, Novartis Pharmaceuticals Corporation, East Hanover, NJ, USA.
Abstract
Antiviral therapy is needed to address acute coronavirus disease. EGT710 is a novel low-molecular-weight inhibitor of the coronavirus main protease (Mpro). This first-in-human study evaluated the safety, tolerability, and pharmacokinetics of EGT710 in healthy adults. The study conducted in the Netherlands involved three parts: a blinded, placebo-controlled, 3:1 randomized, single ascending dose Part A (n = 39); a multiple ascending dose Part B (n = 31); and an open-label, three-period, six sequence, randomized, cross-over Part C (n = 18) to evaluate food and formulation effects on EGT710 bioavailability. EGT710 was well tolerated. All adverse events (AEs) were mild (Grade 1), with no serious AEs or discontinuations. Aside from mild gastrointestinal AEs associated with EGT710, AE frequency was similar between groups with no dose-dependent or dose-limiting adverse effects. EGT710 was rapidly absorbed (median Tmax 2.0 h), showed sub-proportional AUC and Cmax increases and no significant accumulation with daily dosing. Bioavailability was comparable between suspension and capsule formulations. Food increased Cmax by 20% and AUC by 27%. EGT710 700 mg once daily for 7 days modestly induced CYP3A4 activity but had no effect on organic anion transporting polypeptide (OAT1/3) activity. Oral EGT710 (capsule and suspension) was safe and well tolerated, with pharmacokinetics that support further development as a treatment for coronavirus disease.
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BibTeX
@article{oosterhaven2026safety,
title = {{Safety, Tolerability, and Pharmacokinetics of EGT710, a Novel Coronavirus Mpro Inhibitor, in Healthy Adults: A Randomized, Single- and Multiple-Dose Study.}},
author = {Jart A F Oosterhaven and Jonathan Trolander and Lidiya Bebrevska and Hilmar Schiller and Begum Alaybeyoglu and Suzanne Gaudet and Allison Claas and Kamal Kumar Balavenkatraman and Renee Bergeron and Fernanda V Duraes and Frederique Chaperon and Swati Ghanshani and Elisabete Goncalves and Steven J Kovacs},
journal = {Clinical pharmacology in drug development},
year = {2026},
month = oct,
doi = {10.1002/cpdd.70115},
url = {https://europepmc.org/article/MED/42925259},
note = {CC BY},
}
RIS
TY - JOUR
TI - Safety, Tolerability, and Pharmacokinetics of EGT710, a Novel Coronavirus Mpro Inhibitor, in Healthy Adults: A Randomized, Single- and Multiple-Dose Study.
AU - Jart A F Oosterhaven
AU - Jonathan Trolander
AU - Lidiya Bebrevska
AU - Hilmar Schiller
AU - Begum Alaybeyoglu
AU - Suzanne Gaudet
AU - Allison Claas
AU - Kamal Kumar Balavenkatraman
AU - Renee Bergeron
AU - Fernanda V Duraes
AU - Frederique Chaperon
AU - Swati Ghanshani
AU - Elisabete Goncalves
AU - Steven J Kovacs
PY - 2026
DA - 2026/10/01
JO - Clinical pharmacology in drug development
DO - 10.1002/cpdd.70115
UR - https://europepmc.org/article/MED/42925259
AB - Antiviral therapy is needed to address acute coronavirus disease. EGT710 is a novel low-molecular-weight inhibitor of the coronavirus main protease (Mpro). This first-in-human study evaluated the safety, tolerability, and pharmacokinetics of EGT710 in healthy adults. The study conducted in the Netherlands involved three parts: a blinded, placebo-controlled, 3:1 randomized, single ascending dose Part A (n = 39); a multiple ascending dose Part B (n = 31); and an open-label, three-period, six sequence, randomized, cross-over Part C (n = 18) to evaluate food and formulation effects on EGT710 bioavailability. EGT710 was well tolerated. All adverse events (AEs) were mild (Grade 1), with no serious AEs or discontinuations. Aside from mild gastrointestinal AEs associated with EGT710, AE frequency was similar between groups with no dose-dependent or dose-limiting adverse effects. EGT710 was rapidly absorbed (median Tmax 2.0 h), showed sub-proportional AUC and Cmax increases and no significant accumulation with daily dosing. Bioavailability was comparable between suspension and capsule formulations. Food increased Cmax by 20% and AUC by 27%. EGT710 700 mg once daily for 7 days modestly induced CYP3A4 activity but had no effect on organic anion transporting polypeptide (OAT1/3) activity. Oral EGT710 (capsule and suspension) was safe and well tolerated, with pharmacokinetics that support further development as a treatment for coronavirus disease.
SN - 2160-763X
SN - 2160-7648
ER -