Indications
Nintedanib capsule is used in adults for the treatment of Idiopathic Pulmonary Fibrosis (IPF). It is also used in adults for the treatment of chronic fibrosing interstitial lung diseases (ILDs) with a progressive phenotype, and in adults for the treatment of systemic sclerosis-associated interstitial lung disease (SSc-ILD). Nintedanib is also indicated in combination with docetaxel for adult patients with locally advanced, metastatic or locally recurrent non-small cell lung cancer (NSCLC) of adenocarcinoma tumor histology, after first-line chemotherapy.
⚠️ Always consult a registered physician before taking any medicine.
Pharmacology
Nintedanib is a small molecule, competitive, triple angiokinase inhibitor. It targets several receptor tyrosine kinases (RTKs) and non-receptor tyrosine kinases (nRTKs). Many of these RTKs are involved in lung fibrosis and tumour angiogenesis, so nintedanib is used to treat proliferative diseases such as idiopathic pulmonary fibrosis, non-small cell lung cancer, and systemic sclerosis-associated interstitial lung disease. The RTKs it inhibits are platelet-derived growth factor (PDGFR) α and β, fibroblast growth factor receptor (FGFR) 1 to 3, vascular endothelial growth factor receptor (VEGFR), and Fns-Like tyrosine kinase-3 (FLT3). Nintedanib binds to the ATP-binding pocket of these receptors and blocks their activity. That stops the signalling cascades that lead to the proliferation and migration of lung fibroblasts. It also inhibits kinase signalling pathways in various cells within tumour tissues, including endothelial cells, pericytes, smooth muscle cells, and cells contributing to angiogenesis. The end result is inhibition of cell proliferation and apoptosis of the affected tumour cells. Besides blocking RTKs, nintedanib prevents the actions of the nRTKs Lck, Lyn, and Src. It is unclear how much the inhibition of Lck and Lyn adds to the therapeutic efficacy of nintedanib, but inhibition of the Src pathway has been shown to reduce lung fibrosis.
Pregnancy & Breastfeeding
Women of childbearing potential and contraception
Nintedanib may cause harm to the foetus in humans. Women who could become pregnant should be advised to avoid pregnancy while they are being treated with Nintedanib. They should use adequate contraception during treatment and for at least 3 months after the last dose. No one has studied how Nintedanib affects the metabolism or the efficacy of hormonal contraceptives, so barrier methods should be used as a second form of contraception to avoid pregnancy.
Pregnancy
There is no information on the use of Nintedanib in pregnant women, but pre-clinical studies in animals have shown reproductive toxicity of this active substance. Because Nintedanib may harm the foetus in humans too, it must not be used during pregnancy. Female patients should be told to inform their doctor or pharmacist if they become pregnant during therapy. If a patient does become pregnant while taking Nintedanib, she should be told about the possible hazard to the foetus, and stopping the treatment should be considered.
Lactation
There is no information on whether Nintedanib and its metabolites pass into human milk. Pre-clinical studies showed that small amounts of Nintedanib and its metabolites (≤ 0.5% of the administered dose) were secreted into the milk of lactating rats. A risk to newborns and infants cannot be excluded. Breast-feeding should be stopped during treatment with Nintedanib.
Fertility
Pre-clinical investigations found no evidence of impaired male fertility. Subchronic and chronic toxicity studies also found no evidence that female fertility in rats is impaired at a systemic exposure level comparable with that at the maximum recommended human dose (MRHD) of 150 mg twice daily.
⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
Dosage Reference
⚠️ Reference ranges from official sources only. Consult your doctor for personalized dosing.
Side Effects & Interactions
Side Effects
No side-effect data recorded yet.