Entrectinib is a Small Molecule owned by F. Hoffmann-La Roche, and is involved in 42 clinical trials, of which 20 were completed, and 22 are ongoing.

Entretinib is a low molecular weight compound having an inhibitory action on receptor tyrosine kinases (TRK) TRKA, TRKB, and TRKC (encoded by the neurotrophic tyrosine receptor kinase [NTRK] genes NTRK1, NTRK2, and NTRK3, respectively), proto-oncogene tyrosine-protein kinase ROS1 (ROS1), and anaplastic lymphoma kinase (ALK) with IC50 values of 0.1 to 2 nM. It also inhibits JAK2 and TNK2 with IC50 values > 5 nM. Entretinib inhibits tumor growth by inhibiting the phosphorylation of TRK, ROS1, or ALK kinase domains and thereby inhibiting the hyperactivation of downstream signaling pathways that leads to unconstrained cell proliferation.

RXDX-101 selectively inhibits TrkA, TrkB and TrkC, ROS1 and ALK proteins. Tyrosine kinases acts as key regulators of signaling pathways, controlling cell growth and differentiation. Deregulation of tyrosine kinase–mediated signaling enhances the initiation and progression of disease. The drug candidate blocks the activity of tyrosine kinases and the signaling pathways they activate, thereby exhibiting therapeutic effect.

The revenue for Entrectinib is expected to reach a total of $2.7bn through 2038. This change impacts the valuation of this asset and is an important factor to understand the current value of the drug in a clinical process. View the complete picture with the Entrectinib NPV Report.

Entrectinib is currently owned by F. Hoffmann-La Roche.

Entrectinib Overview

Entrectinib (Rozlytrek) belongs to phenylpiperazines class of compounds, acts as an anti-neoplastic agent. It is formulated as hard gelatin capsules for oral route of administration. Rozlytrek is indicated for the treatment of adult and pediatric patients with neurotrophic tyrosine receptor kinase (NTRK) fusion-positive, advanced recurrent solid tumours including pancreatic cancer, thyroid cancer, salivary gland cancer, breast cancer, colorectal cancer, and non small cell lung cancer, and also indicated for the treatment of TrkA-positive, TrkB-positive, TrkC-positive ROS1-positive or ALK-positive non-small cell lung cancer.

Entrectinib (RXDX-101) is under development for the treatment of solid tumors including non-small cell lung cancer (NSCLC), metastatic colorectal cancer, anaplastic large cell lymphoma, leptomeningeal disease, metastatic pancreatic cancer, salivary gland cancer, brain tumor, astrocytoma, synovial sarcoma, fibrosarcoma, triple negative, HER-2 positive, ER or PR positive breast cancer, head and neck cancer, ovarian cancer, neuroblastoma, central nervous system (CNS) tumor, cholangiocarcinoma, papillary thyroid cancer, renal cell carcinoma, metastatic melanoma, mammary analog secretory carcinoma, acute myeloid leukemia, squamous non-small cell lung cancer and stages I-III non-small cell lung cancer with ALK, ROS1, NTRK, or BRAF v600E molecular alterations. The drug candidate is administered orally. The drug candidate is a selective tyrosine kinase inhibitor of the TrkA, TrkB and TrkC, ROS1 and ALK proteins. It is developed based on Rx/Dx technology platform.

F. Hoffmann-La Roche Overview

F. Hoffmann-La Roche (Roche) is a biotechnology company that develops drugs and diagnostics to treat major diseases. It provides medicines for the treatment of cancer, other auto-immune diseases, central nervous system disorders, ophthalmological disorders, infectious diseases, and respiratory diseases. The company also offers in vitro diagnostics, tissue-based cancer diagnostics, and diabetes management solutions. Roche conducts research to identify novel methods to prevent, diagnose, and treat diseases. The company offers its products and services to hospitals, commercial laboratories, healthcare professionals, researchers, and pharmacists. Together with its subsidiaries and partners, the company has operations in various countries. Roche is headquartered in Basel, Switzerland.

The company reported revenues of (Swiss Francs) CHF62,801 million for the fiscal year ended December 2021 (FY2021), an increase of 7.7% over FY2020. In FY2021, the company’s operating margin was 28.9%, compared to an operating margin of 31.8% in FY2020. In FY2021, the company recorded a net margin of 22.2%, compared to a net margin of 24.5% in FY2020.

Quick View – Entrectinib

Report Segments
  • Innovator (NME)
Drug Name
  • Entrectinib
Administration Pathway
  • Oral
Therapeutic Areas
  • Oncology
Key Companies
Highest Development Stage
  • Marketed

GlobalData, the leading provider of industry intelligence, provided the underlying data, research, and analysis used to produce this article.

To create this model, GlobalData takes into account factors including patent law, known and projected regulatory approval processes, cash flows, potential applicable patients, drug margins, company expenses, and pricing estimates. Combining these data points with GlobalData’s world class analysis creates high value models that companies can use to help in evaluation processes for each drug or company.

The rNPV method integrates the probability of a drug reaching a clinical stage into the cash flow at that time, which provides a more accurate rNPV, as it considers the probability that the drug never makes it through the clinical pathway to commercialization. GlobalData’s rNPV model uses proprietary likelihood of approval (LoA)and phase transition success rate(PTSR) data for the indication in the highest development stage, which can be found on GlobalData’s Pharmaceutical Intelligence Center.