Related Experiment Video
Updated: Jan 7, 2026
Using 22C3 Anti-PD-L1 Antibody Concentrate on Biopsy and Cytology Samples from Non-small Cell Lung Cancer Patients
Published on: September 25, 2018
Ceralasertib, an ATR kinase inhibitor, as monotherapy in Japanese patients with advanced solid malignancies: Results
Yasutoshi Kuboki1, Nobuaki Matsubara2, Hiromichi Nakajima2
1National Cancer Center Hospital East, Chiba, Japan. ykuboki@east.ncc.go.jp.
Background:
Ceralasertib is an oral, selective, and potent inhibitor of ATR serine/threonine kinase, a key protein involved in cell cycle checkpoint regulation and DNA damage response. We report preliminary safety, tolerability, and pharmacokinetic data of ceralasertib monotherapy in Japanese patients with advanced solid tumors.
Methods:
In this phase 1, open-label study, patients orally received ceralasertib twice daily 240 mg on days 1-7 (Cohort 1) or 160 mg on days 1-14 (Cohort 2) of a 28-day cycle, respectively; both cohorts also received a single ceralasertib dose 4 days before Cycle 1. Patients were aged ≥ 18 years with solid malignancies refractory to standard therapies or for which no standard therapy exists. The primary objective was to determine ceralasertib safety; secondary objectives included assessing antitumor activity and pharmacokinetics. Exploratory objectives included biomarker analysis.
Results:
Twelve of 14 patients screened received ceralasertib. At data cutoff (August 17, 2023), all 12 patients had experienced at least one treatment-emergent adverse event (AE; grade ≥ 3, n = 3). One patient in each cohort had a dose-limiting toxicity; no AE-related deaths were reported. In total, 6 patients had a best objective response of stable disease (Cohort 1, n = 2; Cohort 2, n = 4). A trend suggesting dose-proportional increases in exposure following single and multiple administration of ceralasertib was observed.
Conclusion:
Ceralasertib monotherapy was generally well tolerated in Japanese patients with advanced solid tumors. The small number of patients enrolled prevents definitive conclusions on the efficacy of ceralasertib monotherapy to be made.
Trial Registration:
ClinicalTrials.gov, NCT05469919. Registration date: May 18, 2022.
Insights
Ceralasertib, an ATR inhibitor, showed good tolerability in Japanese patients with advanced solid tumors. Preliminary results indicate potential for further investigation in this patient population.
Area of Science:
- Oncology
- Pharmacology
- Clinical Trials
Background:
- Ceralasertib is an oral, selective ATR kinase inhibitor targeting DNA damage response.
- ATR inhibition is crucial for cell cycle checkpoint regulation.
- Advanced solid tumors present challenges in treatment and require novel therapeutic strategies.
Purpose of the Study:
- To evaluate the safety and tolerability of ceralasertib monotherapy in Japanese patients.
- To assess the pharmacokinetic profile of ceralasertib in this population.
- To explore preliminary antitumor activity and biomarker responses.
Main Methods:
- Phase 1, open-label study design.
- Oral administration of ceralasertib at different doses and schedules.
- Inclusion of adult patients with advanced solid malignancies refractory to standard treatments.
Main Results:
- Ceralasertib was generally well-tolerated, with manageable treatment-emergent adverse events.
- Preliminary pharmacokinetic data suggested dose-proportional exposure.
- Stable disease was observed in 6 out of 12 patients, indicating potential clinical activity.
Conclusions:
- Ceralasertib monotherapy demonstrates a favorable safety profile in Japanese patients with advanced solid tumors.
- Further studies are warranted to confirm efficacy due to the limited sample size.
More Related Videos
09:38Establishing Dual Resistance to EGFR-TKI and MET-TKI in Lung Adenocarcinoma Cells In Vitro with a 2-step Dose-escalation Procedure
Published on: August 11, 2017
04:04Endobronchial Ultrasound-guided Intratumoral Injection of Cisplatin for the Treatment of Isolated Mediastinal Recurrence of Lung Cancer
Published on: February 12, 2017
Related Concept Videos
02:56Treatment Resistant Cancers
02:57Targeted Cancer Therapies
There are several types of targeted therapies against...
02:49Cancer Therapies
However, cancer treatments can pose several challenges, as therapies used to kill cancer cells are generally also toxic to normal cells. Moreover, cancer cells mutate rapidly and can develop resistance to chemical agents or radiation therapy. Besides, all types of cancer cells may not respond to the same therapy. Some cancer cells respond to one...
01:27Tumor Immunotherapy
01:29Drugs for Treatment of Ulcerative Colitis in IBD
01:29Drugs for Treatment of Crohn's Disease in IBD Using Immunomodulatory Agents