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Activity of Anlotinib in the Second-Line Therapy of Metastatic Gastrointestinal Stromal Tumors: A Prospective,
Yongjian Zhou1, Chunling Zeng2, Xiaofeng Sun3
1Department of Gastric Surgery, Fujian Medical University Union Hospital, Fujian, People's Republic of China.
Background:
Anlotinib is a multi-target tyrosine kinase inhibitor that can effectively inhibit tumor cell proliferation after receptor kinase activation caused by KIT gene mutation.
Methods:
We tested the inhibitory effect of anlotinib in GIST cell lines with different gene mutations and evaluated the efficacy of anlotinib for patients with metastatic GIST after imatinib failure in a multicenter, single-arm, phase II study.
Results:
In vitro, V654A mutation encoded by KIT exon 13 was intermediately sensitive to anlotinib. Moreover, anlotinib was able to partly suppress the activation loop mutation D820A from exon 17 while another activation loop mutation N822K, also from exon 17, was resistant to anlotinib. From September 2018 to October 2020, 64 patients from 9 Chinese medical centers were enrolled in this study. Seven patients had partial response and 39 patients had stable disease. The median PFS was 8.0 months. There was no statistical significance comparing with PFS of sunitinib second-line therapy at the same period. The most common adverse events related to anlotinib treatment were hypertension, neutropenia, and fatigue.
Conclusion:
Anlotinib showed moderate antitumor activity in drug-resistant GIST cell lines in vitro, and good PFS and better tolerance in second-line therapy study.
Insights
Anlotinib demonstrates moderate efficacy against drug-resistant gastrointestinal stromal tumor (GIST) cell lines. In a phase II study, it showed a median progression-free survival of 8.0 months in patients with metastatic GIST.
Area of Science:
- Oncology
- Pharmacology
- Genetics
Background:
- Anlotinib is a multi-target tyrosine kinase inhibitor.
- It targets KIT gene mutations, which drive tumor cell proliferation in GIST.
- GIST is a challenging cancer, especially after imatinib treatment failure.
Purpose of the Study:
- To evaluate anlotinib's inhibitory effect on GIST cell lines with various gene mutations.
- To assess anlotinib's efficacy in metastatic GIST patients who failed imatinib therapy.
- To determine the safety and tolerability of anlotinib in this patient population.
Main Methods:
- In vitro testing of anlotinib on GIST cell lines with different KIT gene mutations.
- A multicenter, single-arm, phase II clinical study involving 64 patients with metastatic GIST.
- Evaluation of progression-free survival (PFS) and adverse events.
Main Results:
- Anlotinib showed intermediate sensitivity to KIT exon 13 V654A mutation and partial suppression of exon 17 D820A mutation.
- KIT exon 17 N822K mutation exhibited resistance to anlotinib.
- Median PFS was 8.0 months; common adverse events included hypertension, neutropenia, and fatigue.
Conclusions:
- Anlotinib exhibits moderate antitumor activity in vitro against drug-resistant GIST cell lines.
- The drug demonstrated a good PFS and better tolerance in second-line therapy for metastatic GIST.
- Anlotinib represents a potential treatment option for GIST patients post-imatinib failure.
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