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- || TAK-020 / Takeda, Ligand
Clinical, Journal: A Phase I, Randomized, Double-Blind, Placebo-Controlled, Single-Dose and Multiple-Rising-Dose Study of the BTK Inhibitor TAK-020 in Healthy Subjects. (Pubmed Central) - Jan 4, 2022
TAK-020 was generally well-tolerated in healthy subjects after single and multiple doses and demonstrated target engagement and pathway modulation. The PD effects outlasted drug exposures, as expected for covalent inhibition of BTK.
- || TAK-020 / Takeda, Ligand
Clinical, Journal: Discovery of the Bruton's Tyrosine Kinase Inhibitor Clinical Candidate TAK-020 (S)-5-(1-((1-Acryloylpyrrolidin-3-yl)oxy)isoquinolin-3-yl)-2,4-dihydro-3H-1,2,4-triazol-3-one, by Fragment-Based Drug Design. (Pubmed Central) - Dec 16, 2021
This publication details the successful use of FBDD (fragment-based drug discovery) principles in the invention of a novel covalent Bruton's tyrosine kinase inhibitor, which ultimately became the Takeda Pharmaceuticals clinical candidate TAK-020. Described herein are the discovery of the fragment 5-phenyl-2,4-dihydro-3H-1,2,4-triazol-3-one, the subsequent optimization of this hit molecule to the candidate, and synthesis and performance in pharmacodynamic and efficacy models along with direct biophysical comparison of TAK-020 with other clinical-level assets and the marketed drug Ibrutinib.
- ||| TAK-020 / Takeda, Ligand
Trial completion: Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Ascending Single- and Multiple-Doses of TAK-020 in Healthy Volunteers (clinicaltrials.gov) - May 25, 2017
P1, N=120, Completed, Sponsor: Takeda
Described herein are the discovery of the fragment 5-phenyl-2,4-dihydro-3H-1,2,4-triazol-3-one, the subsequent optimization of this hit molecule to the candidate, and synthesis and performance in pharmacodynamic and efficacy models along with direct biophysical comparison of TAK-020 with other clinical-level assets and the marketed drug Ibrutinib. Recruiting --> Completed
- || TAK-020 / Takeda, Ligand
Trial primary completion date: Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Ascending Single- and Multiple-Doses of TAK-020 in Healthy Volunteers (clinicaltrials.gov) - Oct 27, 2016
P1, N=128, Recruiting, Sponsor: Takeda
Recruiting --> Completed Trial primary completion date: Sep 2016 --> May 2017
- | TAK-020 / Takeda, Ligand
Trial completion, Enrollment change: TAK-020 Relative Bioavailability and Food Effect Study in Healthy Participants (clinicaltrials.gov) - Sep 8, 2016
P1, N=26, Completed, Sponsor: Takeda
Trial primary completion date: Sep 2016 --> May 2017 Recruiting --> Completed | N=37 --> 26
- TAK-020 / Takeda, Ligand
Enrollment open: TAK-020 Relative Bioavailability and Food Effect Study in Healthy Participants (clinicaltrials.gov) - Jun 4, 2016
P1, N=37, Recruiting, Sponsor: Takeda
Recruiting --> Completed | N=37 --> 26 Not yet recruiting --> Recruiting
- | TAK-020 / Takeda, Ligand
New P1 trial: TAK-020 Relative Bioavailability and Food Effect Study in Healthy Participants (clinicaltrials.gov) - Mar 30, 2016
P1, N=37, Not yet recruiting, Sponsor: Takeda
- || TAK-020 / Takeda, Ligand
Enrollment change, Trial primary completion date: Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Ascending Single- and Multiple-Doses of TAK-020 in Healthy Volunteers (clinicaltrials.gov) - Mar 22, 2016
P1, N=136, Recruiting, Sponsor: Takeda
Not yet recruiting --> Recruiting N=88 --> 136 | Trial primary completion date: Feb 2016 --> Sep 2016
- ||| TAK-020 / Takeda, Ligand
Enrollment open: Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Ascending Single- and Multiple-Doses of TAK-020 in Healthy Volunteers (clinicaltrials.gov) - May 9, 2015
P1, N=88, Recruiting, Sponsor: Takeda
N=88 --> 136 | Trial primary completion date: Feb 2016 --> Sep 2016 Not yet recruiting --> Recruiting
- ||| TAK-020 / Takeda, Ligand
New P1 trial: Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Ascending Single- and Multiple-Doses of TAK-020 in Healthy Volunteers (clinicaltrials.gov) - Apr 9, 2015
P1, N=88, Not yet recruiting, Sponsor: Takeda