Nintedanib is an oral medication used to manage specific lung conditions characterized by scarring of the lung tissue. It is taken as a capsule and is intended to slow the advancement of these serious respiratory illnesses.
Conditions Treated by Nintedanib
One of the primary conditions nintedanib is used for is idiopathic pulmonary fibrosis (IPF). IPF is a disease with an unknown cause where scar tissue builds up in the lungs, leading to shortness of breath and a persistent dry cough. The goal of nintedanib in IPF is to slow the rate at which lung function declines.
Another condition treated with this medication is systemic sclerosis-associated interstitial lung disease (SSc-ILD). Systemic sclerosis, also known as scleroderma, is an autoimmune disease that can affect various parts of the body, including the lungs, causing fibrosis. For these patients, nintedanib helps to slow the loss of pulmonary function.
The drug is also indicated for other chronic fibrosing ILDs with a progressive phenotype, where the disease worsens over time. This includes ILDs where, despite treatment for the underlying cause, lung fibrosis continues to advance.
Finally, nintedanib is used in oncology as part of a combination therapy. It is prescribed alongside another chemotherapy agent, docetaxel, for a specific type of lung cancer. This treatment is for patients with locally advanced, metastatic, or locally recurrent non-small cell lung cancer (NSCLC) of adenocarcinoma histology after initial chemotherapy has failed.
Mechanism of Action
Nintedanib functions as a small molecule tyrosine kinase inhibitor (TKI). Tyrosine kinases are enzymes that act as on/off switches for many cellular functions, including growth and differentiation. In certain diseases, these signaling pathways become overactive, contributing to the disease process. Nintedanib works by blocking several of these enzymes at once.
The drug specifically targets three main groups of tyrosine kinase receptors: vascular endothelial growth factor receptors (VEGFR), fibroblast growth factor receptors (FGFR), and platelet-derived growth factor receptors (PDGFR). These receptors are located on the surface of cells and, when activated, trigger internal signaling cascades. By inhibiting them, nintedanib disrupts the processes that lead to the proliferation and migration of fibroblasts, the cells responsible for producing scar tissue.
This blockage of signaling pathways slows the formation of fibrosis within the lungs. In cancer treatment, inhibiting these receptors also interferes with angiogenesis, the process by which tumors form new blood vessels. This dual action makes it a targeted therapy for its approved conditions.
Common Side Effects and Management
The use of nintedanib is frequently associated with gastrointestinal side effects. Diarrhea is the most common adverse reaction, affecting a significant number of patients. Other prevalent issues include nausea, vomiting, abdominal pain, decreased appetite, and subsequent weight loss. Headaches have also been reported.
Managing these side effects is an important part of treatment. For diarrhea, healthcare providers may recommend maintaining adequate hydration and using over-the-counter anti-diarrheal medications. Patients should communicate any side effects to their doctor, as dose adjustments may be needed to improve tolerance.
Important Safety Information
One of the primary concerns with nintedanib is the potential for liver injury. Patients will undergo blood tests to check liver function before starting the medication and at regular intervals during treatment. Symptoms like yellowing skin or eyes, dark urine, or pain in the upper right abdomen should be reported to a doctor immediately.
The medication can also increase the risk of serious gastrointestinal problems, including a tear in the stomach or intestinal wall, known as perforation. This risk is higher in individuals who have had recent abdominal surgery. There is also an increased chance of bleeding problems and the formation of blood clots, which could lead to a heart attack or stroke.
Nintedanib can harm a developing fetus and should not be used during pregnancy. Women who can become pregnant must have a negative pregnancy test before starting and use effective contraception during treatment. Certain medications and foods can interact with nintedanib, as drugs that affect the CYP3A4 and P-gp pathways can alter its levels in the body.
Administration and Dosage
The standard dosage is one capsule taken twice daily, approximately 12 hours apart. It is recommended to take the medication with food to help with its absorption.
Capsules must be swallowed whole with liquid and should not be chewed, crushed, or opened. Breaking the capsule can alter how the medication is absorbed and can expose the person administering it to the contents. The available capsule strengths are 100 mg and 150 mg.
If a dose is missed, the recommended course of action is to skip that dose entirely and take the next scheduled dose at the regular time. It is important not to take a double dose to make up for the missed one. In the event of an overdose, individuals should contact their doctor or a poison control center for guidance.