Pharmacokinetic characteristics of vactosertib, a new activin receptor-like kinase 5 inhibitor, in patients with advanced solid tumors in a first-in-human phase 1 study
Abstract
Purposes Vactosertib is a new investigational inhibitor of activin receptor-like kinase 5. The objective of this study was to characterize vactosertib pharmacokinetics that are to be applied for subsequent clinical studies. Methods Vactosertib plasma concentration-time data were obtained from a multicenter, dose-escalation, first-in-human phase 1 study conducted in patients with advanced solid tumors. Each patient orally received a fixed dose of vactosertib with the range of 30 mg to 340 mg once daily under fasted condition. Pharmacokinetic analysis was performed using a non-compartmental method. Results Pharmacokinetic data were evaluable in 29 patients. Vactosertib was rapidly absorbed after the first dose with a median time to maximum concentration (t max) of 1.2 h (interquartile range, 0.8-1.8 h) and quickly eliminated with a median terminal half-life (t 1/2) of 3.2 h (2.2-4.2 h) over the dose range studied. Such trend was also observed after repeated doses for five days (median t max, 1.5 h; median t 1/2, 3.0 h). The area under the concentration-time curve within a dosing interval increased in proportion to dose. The median values of apparent clearance and volume of distribution were 29 L/h (21-44 L/h) and 133 L (77-222 L), respectively. The median accumulation ratio after repeated once-daily doses for five days was 0.87 (0.69-1.07). Conclusions Vactosertib pharmacokinetics were dose-proportional within tested dose range with negligible accumulation when administered once daily for five days. Considering the short half-life, it seems necessary to administer vactosertib twice- or thrice-daily to maintain its concentrations above minimum effective level over a dosing interval.
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Monoclonal antibodies prevent TGF-β receptors from binding ligand.
“Another class of therapeutics comprises monoclonal antibodies that prevent TGF-β receptors from binding ligand145,300.”
From TGFβ biology in cancer progression and immunotherapy (2021) · cites this paper as [300]
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Razabdouski, T. N., Dalton, R., Calescibetta, A. R., Christiansen, S., Ward, G., Augello, A. C., Moon, J., Yun, S., Vincelette, N. D., Wright, G. M., et al. (2026) · Cells · doi:10.3390/cells15181674
Zhao, X., Shen, L., Gong, Z., Lv, M., Zhang, Y., Tang, B., & Li, X. (2026) · Oncology Letters · doi:10.3892/ol.2026.15878
Xiang, Z., Li, J., Xu, Y., Xu, C., Li, S., Zheng, S., Yang, Z., Wei, X., & Xu, X. (2026) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-026-03059-8
- Authors
- Jung, S. Y., Hwang, S., Clarke, J. M., Bauer, T. M., Keedy, V. L., Lee, H., Park, N., Kim, S.-J., & Lee, J. I.
- Affiliations
- Seoul National University (KR)
- Duke Medical Center (US)
- Sarah Cannon (US)
- Vanderbilt-Ingram Cancer Center (US)
- National Cancer Center (KR)
- Corresponding author
- Lee, Jangik I.
- Venue
- Investigational New Drugs
- Published
- 2019-07-13
- Volume
- 38
- Issue
- 3
- Pages
- 812-820
- ISSN
- 0167-6997 (ISSN-L)
- 1573-0646
- OpenAlex
- W2958406986
- Cited by
- 69
- References
- 27
- Citations by year
- 2026: 6 · 2025: 12 · 2024: 10 · 2023: 8 · 2022: 16 · 2021: 10 · 2020: 6 · 2019: 1
- FWCI
- 2.73
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- Locations
- Investigational New Drugs (publishedVersion)
- PubMed (publishedVersion)
- Seoul National University Open Repository (Seoul National University) (submittedVersion)
- Funders
- MedPacto, Inc.
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › TGF-β signaling in diseases
- Health Sciences › Medicine › Pediatrics, Perinatology and Child Health › Pharmaceutical studies and practices
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
- Keywords
- vactosertib, ALK5 inhibitor, pharmacokinetics, dose proportionality, oral administration, advanced solid tumors, dosing interval, clearance, volume of distribution
- MeSH terms
- Receptor, Transforming Growth Factor-beta Type I, Administration, Oral, Adult, Aged, Aged, 80 and over, Aniline Compounds, Drug Administration Schedule, Female, Half-Life, Humans, Male, Middle Aged, Neoplasms, Triazoles, Area Under Curve
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