Entrectinib Drugbank: Unpacking a Key Targeted Cancer Therapy

For those researching pharmaceutical compounds, databases like DrugBank serve as invaluable resources, providing detailed scientific and clinical information. When exploring "Entrectinib Drugbank," the intent is often to delve into the intricate specifics of this targeted therapy, understanding its mechanism, applications, and pharmacological profile as cataloged within this comprehensive bioinformatics resource.

Entrectinib is a crucial medication in the oncology landscape, representing a class of drugs designed to specifically target molecular drivers of certain cancers. Its inclusion and detailed description in DrugBank highlight its significance and the wealth of data available for researchers, healthcare professionals, and students.

What is Entrectinib?

Entrectinib is an oral, selective tyrosine kinase inhibitor (TKI) approved for the treatment of specific types of cancer. It works by blocking the activity of certain proteins that are mutated or overexpressed in cancer cells, thereby inhibiting their growth and proliferation. Unlike traditional chemotherapy that broadly targets rapidly dividing cells, Entrectinib offers a more precise approach, focusing on the genetic alterations driving the malignancy.

As detailed in DrugBank, Entrectinib's chemical structure and properties are meticulously documented, providing a foundation for understanding its interactions within biological systems. Its classification as a TKI immediately signals its mechanism-based approach to cancer treatment.

Mechanism of Action: How Entrectinib Works

The primary mechanism of action for Entrectinib involves inhibiting the activity of the anaplastic lymphoma kinase (ALK), ROS1 (ROS proto-oncogene 1, receptor tyrosine kinase), and neurotrophic tyrosine receptor kinase (NTRK) proteins. These fusion proteins or mutations involving ALK, ROS1, or NTRK genes can lead to uncontrolled cell growth and survival, characteristic of various cancers.

By binding to the ATP-binding site of these kinases, Entrectinib prevents their activation, effectively shutting down the signaling pathways that promote cancer cell proliferation and survival. This targeted inhibition is what makes Entrectinib particularly effective in patients whose tumors harbor these specific genetic rearrangements, as thoroughly explained in DrugBank's molecular interaction data.

Approved Indications: When is Entrectinib Used?

DrugBank specifies the approved indications for Entrectinib, which are critical for its clinical application. It is primarily used for the treatment of adult and pediatric patients with solid tumors that have a neurotrophic tyrosine receptor kinase (NTRK) gene fusion, are locally advanced or metastatic, and for which surgical resection is likely to result in severe morbidity, or who have progressed on prior therapy or have no satisfactory alternative treatment.

Additionally, Entrectinib is indicated for the treatment of adult patients with ROS1-positive metastatic non-small cell lung cancer (NSCLC). These precise indications underscore the importance of genetic testing in identifying eligible patients, aligning with the principles of precision medicine.

Pharmacology and Pharmacokinetics

The DrugBank entry for Entrectinib provides extensive data on its pharmacology and pharmacokinetics, crucial aspects for understanding its behavior in the body. This includes information on its absorption, distribution, metabolism, and excretion (ADME) profile. Entrectinib is administered orally, and its absorption characteristics influence its bioavailability and dosing regimens.

Metabolism primarily occurs in the liver, largely mediated by the cytochrome P450 3A (CYP3A) enzyme system, which is a key consideration for potential drug-drug interactions. Its elimination pathways and half-life are also detailed, informing clinicians about dosing frequency and potential accumulation, ensuring optimal therapeutic effects while minimizing adverse reactions.

DrugBank's Role in Understanding Entrectinib

DrugBank serves as an essential bridge between chemical data, pharmacological information, and clinical application. For Entrectinib, it compiles a wealth of data that goes beyond basic facts. Researchers can find detailed chemical identifiers, protein targets, enzyme interactions, and pathways affected by the drug. It also often includes links to clinical trials, adverse event profiles, and drug-drug interaction warnings.

This comprehensive approach allows users to gain a holistic understanding of Entrectinib, from its molecular structure to its therapeutic potential and safety considerations, making it a cornerstone resource for drug discovery and medical education.

Potential Side Effects and Safety Profile

Like all medications, Entrectinib carries a risk of side effects, which are thoroughly documented in resources like DrugBank. Common adverse reactions can include fatigue, constipation, dysgeusia (taste disturbance), dizziness, edema, and weight gain. More serious, though less common, side effects may involve central nervous system effects, heart problems, liver toxicity, and vision changes.

The detailed safety profile available through DrugBank helps healthcare providers anticipate and manage potential adverse events, ensuring patient safety. It emphasizes the importance of careful monitoring throughout the course of treatment to mitigate risks effectively.

Summary

Entrectinib represents a significant advancement in targeted cancer therapy, offering a precise treatment option for patients with specific genetic alterations. Its comprehensive profile within DrugBank provides an invaluable resource for understanding its mechanism of action, approved indications, pharmacokinetic properties, and safety considerations. By leveraging such detailed information, researchers and clinicians can continue to optimize its use, further advancing the field of precision oncology and improving patient outcomes.