| Phase 1/2a Study of Rivoceranib, a Selective VEGFR-2 Angiogenesis Inhibitor, in Patients with Advanced Solid Tumors |
Yoon-Koo Kang1
, Min-Hee Ryu1, Yong Sang Hong1, Chang-Min Choi1, Tae Won Kim1, Baek-Yeol Ryoo1, Jeong Eun Kim1, John R. Weis2, Rachel Kingsford2, Cheol Hee Park3, Seong Jang3, Arlo McGinn3, Theresa L. Werner2, Sunil Sharma4 |
1Department of Oncology, Asan Medical Center, University of Ulsan College of Medicine, Seoul, Korea
2University of Utah and Huntsman Cancer Institute, Salt Lake City, UT, USA
3Elevar Therapeutics, Fort Lee, NJ, USA
4Translational Genomics Research Institute, Phoenix, AZ, USA
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| Correspondence |
Yoon-Koo Kang ,Tel: 82-2-3010-3230, Fax: 82-2-3010-8772, Email: ykkang@amc.seoul.kr
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Received: August 29, 2023; Accepted: January 17, 2024. Published online: January 18, 2024. |
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| ABSTRACT |
Purpose
To report the results from an early-phase study of rivoceranib, an oral tyrosine kinase inhibitor highly selective for vascular endothelial growth factor receptor 2, in patients with advanced solid tumors.
Materials and Methods
In this open-label, single-arm, dose-escalating, multicenter three-part phase 1/2a trial, patients had advanced solid tumors refractory to conventional therapy. Part 1 evaluated the safety and pharmacokinetics of five ascending once-daily doses of rivoceranib from 81 mg to 685 mg. Part 2 evaluated the safety and antitumor activity of once-daily rivoceranib 685 mg. Part 3 was conducted later, due to lack of MTD determination in part 1, to evaluate the safety and preliminary efficacy of once-daily rivoceranib 805 mg in patients with unresectable or advanced gastric cancer.
Results
A total of 61 patients were enrolled in parts 1 (n=25), 2 (n=30), and 3 (n=6). In parts 1 and 2, patients were white (45.5%) or Asian (54.5%), and 65.6% were male. The most common grade ≥3 adverse events (AEs) were hypertension (32.7%), hyponatremia (10.9%), and hypophosphatemia (10.9%). The overall response rate (ORR) was 15.2%. In part 3, dose-limiting toxicities occurred in 2 out of 6 patients: grade 3 febrile neutropenia decreased appetite, and fatigue. The ORR was 33%.
Conclusion
The recommended phase 2 dose of rivoceranib was determined to be 685 mg once daily, which showed adequate efficacy with a manageable safety profile. (NCT01497704 and NCT02711969) |
| Key words:
Apatinib, Rivoceranib, Stomach neoplasms, Solid tumors |
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