Entrectinib (Rxdx-101) Clinical Trials

Size	Price	Qty
5mg	USD 147
25mg	USD 377

Clinical Trials

Numerous clinical trials evaluate the therapeutic profile, pharmacokinetics, and clinical efficacy of entrectinib across Early Phase 1 to Phase 3 studies. These investigations target diverse populations, including patients with advanced solid tumors, non-small cell lung cancer, ER-positive/HER2-negative breast carcinoma, and hematological malignancies, as well as cohorts with hepatic insufficiency and healthy volunteers. Sponsored by major pharmaceutical corporations and academic entities, these studies span recruitment statuses ranging from completed and active to currently recruiting and not yet recruiting.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05862285	RECRUITING	Cancer	Hoffmann-La Roche	2023-06-01	PHASE3
NCT04589845	ACTIVE_NOT_RECRUITING	Solid Tumors	Hoffmann-La Roche	2021-01-18	PHASE2
NCT05170204	ACTIVE_NOT_RECRUITING	Non-Small Cell Lung Cancer	Hoffmann-La Roche	2022-11-01	PHASE3
NCT05722886	RECRUITING	Haematological Malignancy; Solid Tumour	Cancer Research UK	2023-03-01	PHASE2; PHASE3
NCT05770544	RECRUITING	Haematological Malignancy; Malignancy; Malignant Neoplasm; Lymphoproliferative Disorders; Neoplasms by Histologic Type; Neoplasms by Site; Cancer; Brain Neoplasms; Melanoma; Glioma; Solid Tumour	Cancer Research UK	2025-11-30	PHASE2; PHASE3
NCT06692491	NOT_YET_RECRUITING	Rare Tumour	Peking University Shenzhen Hospital	2025-01-01	PHASE2
NCT06528691	RECRUITING	High Grade Glioma; CNS Tumor	St. Jude Children's Research Hospital	2026-05-01	PHASE2
NCT02925234	RECRUITING	Cancer; Tumors; Neoplasm; Neoplasia	The Netherlands Cancer Institute	2016-08	PHASE2
NCT02568267	ACTIVE_NOT_RECRUITING	Breast Cancer; Cholangiocarcinoma; Colorectal Cancer; Head and Neck Neoplasms; Lymphoma, Large-Cell, Anaplastic; Melanoma; Neuroendocrine Tumors; Non-Small Cell Lung Cancer; Ovarian Cancer; Pancreatic Cancer; Papillary Thyroid Cancer; Primary Brain Tumors; Renal Cell Carcinoma; Sarcomas; Salivary Gland Cancers; Adult Solid Tumor	Hoffmann-La Roche	2015-11-19	PHASE2
NCT03178552	ACTIVE_NOT_RECRUITING	Non-Small Cell Lung Cancer	Hoffmann-La Roche	2017-09-22	PHASE2; PHASE3
NCT06195228	RECRUITING	Advanced Thyroid Cancer Patients Who Received Target Therapy	Fudan University	2020-01-01	PHASE4
NCT04302025	RECRUITING	Non-small Cell Lung Cancer	Genentech, Inc.	2020-11-06	PHASE2
NCT05159245	RECRUITING	Advanced Cancer; Solid Tumor; Haematological Malignancy	Helsinki University Central Hospital	2021-12-10	PHASE2
NCT03994796	ACTIVE_NOT_RECRUITING	CDK Gene Mutation; Metastatic Malignant Neoplasm in the Brain; Metastatic Malignant Solid Neoplasm; NTRK Family Gene Mutation; PI3K Gene Mutation; ROS1 Gene Mutation; KRAS G12C Mutation	Alliance for Clinical Trials in Oncology	2019-10-17	PHASE2
NCT04603807	ACTIVE_NOT_RECRUITING	Carcinoma, Non-Small-Cell Lung	Hoffmann-La Roche	2021-09-30	PHASE3
NCT02650401	ACTIVE_NOT_RECRUITING	Solid Tumors; CNS Tumors	Hoffmann-La Roche	2016-05-03	PHASE1; PHASE2
NCT05238831	WITHDRAWN	Advanced Breast Carcinoma; Advanced Malignant Solid Neoplasm; Advanced Ovarian Carcinoma; Advanced Pancreatic Carcinoma; Advanced Prostate Carcinoma; Advanced Sarcoma; Anatomic Stage III Breast Cancer AJCC v8; Anatomic Stage IV Breast Cancer AJCC v8; Recurrent Adult Soft Tissue Sarcoma; Recurrent Breast Carcinoma; Recurrent Ovarian Carcinoma; Recurrent Prostate Carcinoma; Stage II Pancreatic Cancer AJCC v8; Stage III Ovarian Cancer AJCC v8; Stage III Pancreatic Cancer AJCC v8; Stage IV Ovarian Cancer AJCC v8; Stage IV Pancreatic Cancer AJCC v8	OHSU Knight Cancer Institute	2023-01-30	EARLY_PHASE1
NCT04551495	UNKNOWN	Invasive Lobular Breast Carcinoma; ER+ Breast Cancer; HER2-negative Breast Cancer	Jules Bordet Institute	2021-01-14	PHASE2
NCT06482086	RECRUITING	Locally Advanced Thyroid Gland Carcinoma	West China Hospital	2021-06-01	PHASE2
NCT04591431	UNKNOWN	Breast Cancer; Gastrointestinal Cancer; Non Small Cell Lung Cancer; Other Cancer	Fondazione per la Medicina Personalizzata	2020-10-07	PHASE2
NCT05396859	ACTIVE_NOT_RECRUITING	Acute Myeloid Leukemia; Recurrent Acute Myeloid Leukemia; Refractory Acute Myeloid Leukemia	OHSU Knight Cancer Institute	2022-10-28	PHASE1
NCT05770544	Recruiting	Solid Tumor\|Haematological Malignancy\|Malignancy\|Malignant Neoplasm\|Lymphoproliferative Disorders\|Neoplasms by Histologic Type\|Neoplasms by Site\|Cancer\|Brain Neoplasms\|Melanoma\|Glioma	Cancer Research UK\|University of Manchester\|University of Birmingham\|Royal Marsden NHS Foundation Trust\|Hoffmann-La Roche	2024-06	Phase 2\|Phase 3
NCT04632992	COMPLETED	Advanced Unresectable or Metastatic Solid Malignancy	Genentech, Inc.	2021-01-13	PHASE2
NCT03498521	COMPLETED	Cancer of Unknown Primary Site	Hoffmann-La Roche	2018-07-10	PHASE2
NCT04589832	TERMINATED	Uveal Melanoma	Arkadiusz Z. Dudek, MD	2021-01-11	PHASE1; PHASE2
NCT04226833	COMPLETED	Hepatic Insufficiency	Hoffmann-La Roche	2020-02-11	PHASE1
NCT04551495	Recruiting	Invasive Lobular Breast Carcinoma\|ER+ Breast Cancer\|HER2-negative Breast Cancer	Jules Bordet Institute\|Hoffmann-La Roche	2021-01-14	Phase 2
NCT03878524	TERMINATED	Accelerated Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive; Anatomic Stage IV Breast Cancer AJCC v8; Anemia; Ann Arbor Stage III Hodgkin Lymphoma; Ann Arbor Stage III Non-Hodgkin Lymphoma; Ann Arbor Stage IV Hodgkin Lymphoma; Ann Arbor Stage IV Non-Hodgkin Lymphoma; Atypical Chronic Myeloid Leukemia, BCR-ABL1 Negative; Blast Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive; Castration-Resistant Prostate Carcinoma; Chronic Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive; Hematopoietic and Lymphoid System Neoplasm; Locally Advanced Pancreatic Adenocarcinoma; Metastatic Breast Carcinoma; Metastatic Malignant Solid Neoplasm; Metastatic Pancreatic Adenocarcinoma; Myelodysplastic/Myeloproliferative Neoplasm With Ring Sideroblasts and Thrombocytosis; Myelodysplastic/Myeloproliferative Neoplasm, Unclassifiable; Primary Myelofibrosis; Recurrent Acute Lymphoblastic Leukemia; Recurrent Acute Myeloid Leukemia; Recurrent Chronic Lymphocytic Leukemia; Recurrent Chronic Myelogenous Leukemia, BCR-ABL1 Positive; Recurrent Hematologic Malignancy; Recurrent Hodgkin Lymphoma; Recurrent Myelodysplastic Syndrome; Recurrent Myelodysplastic/Myeloproliferative Neoplasm; Recurrent Myeloproliferative Neoplasm; Recurrent Non-Hodgkin Lymphoma; Recurrent Plasma Cell Myeloma; Recurrent Small Lymphocytic Lymphoma; Refractory Acute Lymphoblastic Leukemia; Refractory Acute Myeloid Leukemia; Refractory Chronic Lymphocytic Leukemia; Refractory Chronic Myelogenous Leukemia, BCR-ABL1 Positive; Refractory Chronic Myelomonocytic Leukemia; Refractory Hematologic Malignancy; Refractory Hodgkin Lymphoma; Refractory Malignant Solid Neoplasm; Refractory Myelodysplastic Syndrome; Refractory Myelodysplastic/Myeloproliferative Neoplasm; Refractory Non-Hodgkin Lymphoma; Refractory Plasma Cell Myeloma; Refractory Primary Myelofibrosis; Refractory Small Lymphocytic Lymphoma; Stage II Pancreatic Cancer AJCC v8; Stage III Pancreatic Cancer AJCC v8; Stage IV Pancreatic Cancer AJCC v8; Stage IV Prostate Cancer AJCC v8; Unresectable Pancreatic Adenocarcinoma	OHSU Knight Cancer Institute	2020-04-01	PHASE1
NCT02097810	COMPLETED	Locally Advanced Solid Tumors; Metastatic Solid Tumors	Hoffmann-La Roche	2014-07-28	PHASE1
NCT04226833	Completed	Hepatic Insufficiency	Hoffmann-La Roche	2020-02-11	Phase 1
NCT03961100	COMPLETED	Solid Tumor	Genentech, Inc.	2019-06-06	PHASE1
NCT03796013	COMPLETED	Healthy Volunteers	Genentech, Inc.	2019-01-10	PHASE1
NCT03796260	COMPLETED	Healthy Volunteers	Genentech, Inc.	2019-01-09	PHASE1
NCT03796013	Completed	Healthy Volunteers	Genentech Inc.	2019-01-10	Phase 1
NCT02587650	TERMINATED	ALK Fusion Protein Expression; BRAF wt Allele; Invasive Skin Melanoma; MET Fusion Gene Positive; NRAS wt Allele; NTRK1 Fusion Positive; NTRK2 Fusion Positive; NTRK3 Fusion Positive; RET Fusion Positive; ROS1 Fusion Positive; Stage III Cutaneous Melanoma; Stage IIIA Cutaneous Melanoma; Stage IIIB Cutaneous Melanoma; Stage IIIC Cutaneous Melanoma; Stage IV Cutaneous Melanoma	University of California, San Francisco	2015-03-26	PHASE2
NCT03330990	COMPLETED	Advanced Solid Tumor	Hoffmann-La Roche	2017-11-14	PHASE1

(data from https://clinicaltrials.gov, updated on 2026-09-02)

Check the Entrectinib (Rxdx-101) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Entrectinib is a potent, orally bioavailable pan-TrkA/B/C, ROS1, and ALK inhibitor with IC50 values ranging from 0.1 to 1.7 nM that selectively binds these receptor tyrosine kinases to suppress downstream oncogenic signaling pathways and stimulate cellular autophagy. By blocking driver tyrosine kinase activity, entrectinib inhibits tumor cell proliferation and induces cell death, providing the biochemical basis for its evaluated clinical efficacy in treating advanced solid tumors and non-small cell lung cancer.

Appendix RUO and cGMP Quality Standards

Quality Dimension	RUO (Research Use Only)	cGMP (Current Good Manufacturing Practice)
Clinical Applicability	Prohibited in human clinical trials or medical diagnostics.	Mandatory for human clinical trials (Phase I–III) and therapies.
Regulatory Status	Non-regulated grade; exempt from drug manufacturing laws.	Legally enforced by health authorities (e.g., FDA, EMA, NMPA).
Facility Environment	Unclassified analytical or research laboratories.	Validated Cleanrooms (ISO Class 5–8) with continuous monitoring.
Quality Control	Basic purity and activity testing.	Rigorous safety release testing (Sterility, Endotoxin, Mycoplasma).
Process Validation	Basic equipment calibration; no process validation required.	Full qualification (IQ/OQ/PQ) and complete batch records.
Quality Assurance	Vendor self-declared without required formal QMS.	Mandatory QA/QC unit, Change Control, CAPA, and vendor audits.
Regulatory Impact	High risk of IND rejection if used as a critical raw material.	Required for IND/NDA filings, supported by Drug Master Files (DMF).

Footnotes

Regulatory Note: Governed by FDA (21 CFR Parts 210/211/312), EMA (EudraLex Vol 4), ICH Guidelines (E6/Q7/Q9/Q10), and compendial standards (USP <71>/<85>/<1043>).