Nintedanib

Antifibrotics
Antifibrotics
Pregnancy: contraindicated
Can harm the fetus. Pregnancy is excluded before treatment and highly effective contraception continues for at least three months after the last dose; breastfeeding is not…

An oral kinase inhibitor that slows lung scarring in idiopathic pulmonary fibrosis and other progressive fibrosing lung diseases; diarrhoea is common.

Updated Nov 1, 2026

Also called: Nintedanib esylate

Quick facts

Group: Antifibrotics
Target: Growth-factor receptor tyrosine kinases (VEGFR, FGFR and PDGFR)
Used for: Idiopathic pulmonary fibrosis
Key effects: Diarrhoea · Nausea · Raised liver enzymes
Monitor: Liver tests · Pregnancy test before starting
ATC: L01EX09

No doses: the clinician sets them by the current guideline.

Mechanism of action

Growth-factor receptor tyrosine kinases (VEGFR, FGFR and PDGFR)Nintedanib

The figure shows nintedanib in the ATP pocket of the human VEGFR2 kinase domain (crystal structure). It blocks the FGF and PDGF receptor kinases in the same way.

Target in 3D: Growth-factor receptor tyrosine kinases (VEGFR, FGFR and PDGFR). PDB structure 3C7Q (RCSB PDB, public domain). View the structure at RCSB PDB

Nintedanib is a small-molecule inhibitor of several receptor tyrosine kinases: the PDGF receptors alpha and beta, FGF receptors 1 to 3 and VEGF receptors 1 to 3, plus some non-receptor kinases. It competes with ATP in the kinase pocket, so the growth-factor signal does not pass into the cell. Lung fibroblasts then proliferate, migrate and turn into collagen-making myofibroblasts less, and the yearly loss of lung function slows.

Growth factors (PDGF, FGF, VEGF) activate fibroblast receptor kinases
Nintedanib occupies the ATP pocket of these kinases
Fibroblasts multiply, migrate and make collagen less
Loss of lung function (FVC) slows; scar is not reversed

Indications

Idiopathic pulmonary fibrosis Interstitial lung disease →
Chronic fibrosing interstitial lung diseases with a progressive phenotype Interstitial lung disease →
Interstitial lung disease associated with systemic sclerosis, to slow the decline in lung function Systemic sclerosis (scleroderma, including CREST) →

Adverse effects

Common

Diarrhoea (very common)
Nausea, vomiting, abdominal pain and decreased appetite
Raised liver enzymes
Weight loss and headache
Hypertension

Contraindications

Pregnancy (fetal harm)
Not recommended in moderate or severe hepatic impairment
Caution with high cardiovascular risk, bleeding risk, recent abdominal surgery or diverticular disease

Key interactions

P-gp and CYP3A4 inhibitors (ketoconazole, erythromycin): Higher nintedanib exposure; patients are watched closely for adverse effects
P-gp and CYP3A4 inducers (rifampicin, carbamazepine, phenytoin, St John's wort): Lower nintedanib exposure; combination avoided
Anticoagulants: Higher bleeding risk; anticoagulation is monitored closely
Oral hormonal contraceptives: May fail when vomiting or diarrhoea reduce absorption; a barrier method is added

What is monitored

Liver tests (ALT, AST, bilirubin) before starting, regularly in the first months and then periodically
Pregnancy test before starting in women who can become pregnant
Diarrhoea, hydration and weight
Urine protein; signs of bleeding in patients on anticoagulants

Administration and safety

Oral capsules taken with food, swallowed whole with liquid
Capsules are not chewed, crushed or opened; skin that touches the contents is washed at once
A missed dose is skipped, not made up

Pregnancy and breastfeeding

Can harm the fetus. Pregnancy is excluded before treatment and highly effective contraception continues for at least three months after the last dose; breastfeeding is not recommended.

Nursing care

Ask about pregnancy plans, bleeding disorders, anticoagulants, heart disease and recent abdominal surgery before starting
Teach early treatment of diarrhoea with fluids and an antidiarrhoeal, and to report persistent diarrhoea
Check liver tests and teach the signs of liver injury: jaundice, dark urine, right upper abdominal pain
Teach the warning signs of bleeding, chest pain and stroke
Advise stopping smoking

Pharmacokinetics

Absorption: Oral capsule taken with food; low absolute bioavailability (about 5%) because of transporters and first-pass metabolism
Distribution: Highly bound to plasma proteins (about 98%), mainly albumin
Metabolism: Mainly hydrolysed by esterases to a free acid, then glucuronidated; CYP3A4 plays a minor role. It is a P-glycoprotein substrate
Elimination: Mainly in faeces via the bile; very little in urine
Half-life: About 9.5 hours (effective half-life in IPF)

Test yourself

Think of the answer, then tap the question to see it.

Which receptor families does nintedanib inhibit?

The tyrosine kinases of the PDGF, FGF and VEGF receptors.

What is the most common adverse effect of nintedanib?

Diarrhoea.

Why is extra care needed when a patient on nintedanib takes an anticoagulant?

Nintedanib raises bleeding risk (it blocks VEGF signalling), so bleeding risk adds up.

Which contraception advice goes with nintedanib?

Highly effective contraception during treatment and for at least three months afterwards, with a barrier method added because diarrhoea or vomiting can make the pill fail.

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Connections

← Back to the class: Antifibrotics

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: DailyMed - NINTEDANIB capsule (DailyMed (U.S. National Library of Medicine), 2026); Nintedanib: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); RCSB PDB - 3C7Q: Structure of VEGFR2 kinase domain in complex with BIBF1120 (RCSB Protein Data Bank, 2008); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.