APG-2449 in Patients With Advanced Solid Tumors
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ClinicalTrials.gov Identifier: NCT03917043 |
Recruitment Status :
Recruiting
First Posted : April 16, 2019
Last Update Posted : October 19, 2020
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Condition or disease | Intervention/treatment | Phase |
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Advanced Solid Cancer Non Small Cell Lung Cancer Esophageal Cancer Ovarian Cancer Malignant Pleural Mesothelioma | Drug: APG-2449 | Phase 1 |
Study Type : | Interventional (Clinical Trial) |
Estimated Enrollment : | 40 participants |
Allocation: | N/A |
Intervention Model: | Sequential Assignment |
Intervention Model Description: | Beginning with 150 mg dose level, and escalating to 300mg, 450mg, 600mg, 750mg, and 900mg dose level sequentially under "3+3" design |
Masking: | None (Open Label) |
Primary Purpose: | Treatment |
Official Title: | A Phase I Study of the Safety, Pharmacokinetic and Pharmacodynamic Properties of Orally Administered APG-2449 in Patients With Advanced Solid Tumors |
Actual Study Start Date : | May 27, 2019 |
Estimated Primary Completion Date : | May 2021 |
Estimated Study Completion Date : | May 2022 |

Arm | Intervention/treatment |
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Experimental: APG-2449
APG-2449 will be explored sequentially using a standard 3+3 escalation scheme at the dose escalation phase and up to 15 patient at the MTD dose level.
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Drug: APG-2449
Capsule, multiple dose cohorts, oral administration every day (QD) of a 28-day cycle
Other Name: APG-2449 Capsule |
- Maximum Tolerated Dose (MTD) [ Time Frame: 28 days ]To determine the maximum tolerated dose (MTD) of APG-2449 in subjects with advanced solid tumors
- Recommended Phase 2 dose (RP2D) [ Time Frame: 28 days ]To determine the tentative recommended Phase 2 dose (RP2D) of APG-2449 in subjects with advanced solid tumors
- Maximum plasma concentration (Cmax) [ Time Frame: 28 days ]Maximum plasma concentration (Cmax) will be assessed on all participants with APG-2449 treatments
- Area under the plasma concentration versus time curve (AUC) [ Time Frame: 28 days ]Area under the plasma concentration versus time curve (AUC) will be assessed on all participants with APG-2449 treatments
- Phosphorylation of FAK protein [ Time Frame: 28 days ]Phosphorylation of FAK protein will be assessed in peripheral blood mononuclear cells on all participants with APG-2449 treatments
- Preliminary efficacy assessment: Response Evaluation Criteria In Solid Tumors (RECIST) 1.1 [ Time Frame: 4 weeks ]To assess preliminary efficacy in subjects with solid tumors using Response Evaluation Criteria In Solid Tumors (RECIST) 1.1

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Ages Eligible for Study: | 18 Years to 75 Years (Adult, Older Adult) |
Sexes Eligible for Study: | All |
Accepts Healthy Volunteers: | No |
Inclusion Criteria:
- Histologically or cytologically confirmed advanced solid tumors that has relapsed from or is refractory to standard treatment, including NSCLC, malignant pleural mesothelioma, esophageal cancer, ovarian cancer, et al.
- ECOG Performance Status ≤ 1.
- Expectation of life ≥ 3 months.
- Adequate hematologic and bone marrow functions.
- Adequate renal and liver function.
- Normal cardiac function.
- Brain metastases with clinically controlled neurologic symptoms.
- Ability to understand and willingness to sign a written informed consent form.
- Willingness to provide tumor samples for testing FAK and p-FAK expression.
Exclusion Criteria:
- Receiving concurrent anti-cancer therapy (chemotherapy, radiotherapy, immunotherapy, biologic therapy); or any investigational therapy within 28 days prior to the first dose of study drug.
- Receiving TKI therapy within 14 days prior to the first dose of study drug.
- Continuance of toxicities due to prior therapy that do not recover (CTCAE V5.0 Grade> 1)
- Has difficulty in swallowing, absorbing barrier, or other diseases blocking APG-2449 ' taken.
- Obvious cardiovascular disease history.
- History of SAE due to prior TKI therapy.
- Failure to recover adequately, as judged by the investigator, from prior surgical procedures. Patients who have had major surgery within 28 days from study entry, and patients who have had minor surgery within 14 days of study entry.
- Active symptomatic fungal, bacterial and/or viral infection including, but not limited to, active human immunodeficiency virus (HIV) or viral hepatitis (B or C).
- Any other condition or circumstance of that would, in the opinion of the investigator, make the patient unsuitable for participation in the study.
- Receiving inhibitors or inducers of CYP3A4, CYP2C9 or CYP2C19 within 7 days prior to the first dose of study drug or during the study.
- Receiving substrates of CYP3A4 with narrow therapy window within 7 days prior to the first dose of study drug or during the study.

To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.
Please refer to this study by its ClinicalTrials.gov identifier (NCT number): NCT03917043
Contact: Yifan Zhai, M.D., Ph.D. | +86-20-28069260 | yzhai@ascentagepharma.com |
China, Guangdong | |
Sun-Yat Sen University Cancer Center | Recruiting |
Guangzhou, Guangdong, China, 510060 | |
Contact: LI ZHANG, Professor +86-20-87343560 Zhangli@sysucc.cn |
Principal Investigator: | Li Zhang, Professor | Sun Yat-sen University |
Responsible Party: | Ascentage Pharma Group Inc. |
ClinicalTrials.gov Identifier: | NCT03917043 |
Other Study ID Numbers: |
APG2449XC101 |
First Posted: | April 16, 2019 Key Record Dates |
Last Update Posted: | October 19, 2020 |
Last Verified: | October 2020 |
Studies a U.S. FDA-regulated Drug Product: | No |
Studies a U.S. FDA-regulated Device Product: | No |
Mesothelioma Neoplasms Adenoma |
Neoplasms, Glandular and Epithelial Neoplasms by Histologic Type Neoplasms, Mesothelial |