Phase I Trial to Evaluate the Tolerance, Pharmacokinetics and Efficacy of the Broad-Spectrum ErbB Family Inhibitor Larotinib Mesylate in Patients With Advanced Solid Tumors
Background: The presented phase I, first-in-human study evaluated the tolerance, pharmacokinetics, and preliminary efficacy of larotinib mesylate in patients with advanced solid tumors.Methods: Cancer patients were assigned to receive larotinib mesylate at 50-400 mg dose levels until disease progres...
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Frontiers Media S.A.,
2021-02-01T00:00:00Z.
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| LEADER | 00000 am a22000003u 4500 | ||
|---|---|---|---|
| 001 | doaj_b51d4c20177744d78a036f1682645d76 | ||
| 042 | |a dc | ||
| 100 | 1 | 0 | |a Jingrui Liu |e author |
| 700 | 1 | 0 | |a Hong Zhang |e author |
| 700 | 1 | 0 | |a Xiaoxue Zhu |e author |
| 700 | 1 | 0 | |a Hong Chen |e author |
| 700 | 1 | 0 | |a Xiaojiao Li |e author |
| 700 | 1 | 0 | |a Yanhua Ding |e author |
| 245 | 0 | 0 | |a Phase I Trial to Evaluate the Tolerance, Pharmacokinetics and Efficacy of the Broad-Spectrum ErbB Family Inhibitor Larotinib Mesylate in Patients With Advanced Solid Tumors |
| 260 | |b Frontiers Media S.A., |c 2021-02-01T00:00:00Z. | ||
| 500 | |a 1663-9812 | ||
| 500 | |a 10.3389/fphar.2021.636324 | ||
| 520 | |a Background: The presented phase I, first-in-human study evaluated the tolerance, pharmacokinetics, and preliminary efficacy of larotinib mesylate in patients with advanced solid tumors.Methods: Cancer patients were assigned to receive larotinib mesylate at 50-400 mg dose levels until disease progression or intolerance. Dose-limiting toxicities were assessed during Cycles 0 and 1. Pharmacokinetic evaluations were performed after the first dose and at steady-state.Results: Twenty-five patients with solid tumors were enrolled in the dose-escalation study. No DLTs were observed. Acne-like rash (68.0%), diarrhea (48.0%), paronychia (48.0%), and anemia (48.0%) were the most reported treatment-related adverse events. No clear linear pharmacokinetic characteristic could be drawn, and obvious accumulation was observed. Two patients with non-small cell lung cancer experienced a partial response, and 15 patients had stable disease after treatment.Conclusion: Continuous oral administration of larotinib mesylate at 50-400 mg daily demonstrated a favorable safety profile, and anti-tumor activity was observed in patients with advanced solid tumors. | ||
| 546 | |a EN | ||
| 690 | |a larotinib | ||
| 690 | |a phase I | ||
| 690 | |a dose escalation | ||
| 690 | |a ErbB family blocker | ||
| 690 | |a pharmacokinetics | ||
| 690 | |a Therapeutics. Pharmacology | ||
| 690 | |a RM1-950 | ||
| 655 | 7 | |a article |2 local | |
| 786 | 0 | |n Frontiers in Pharmacology, Vol 12 (2021) | |
| 787 | 0 | |n https://www.frontiersin.org/articles/10.3389/fphar.2021.636324/full | |
| 787 | 0 | |n https://doaj.org/toc/1663-9812 | |
| 856 | 4 | 1 | |u https://doaj.org/article/b51d4c20177744d78a036f1682645d76 |z Connect to this object online. |