Afatinib

Uses	Advanced or metastatic non-small cell lung cancer
Therapy	Anti-Neoplastic
Side Effects	Diarrhoea, skin rash, mouth sores, nail inflammation

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Molecule Description

Afatinib is an anticancer medicine. It belongs to a class of drugs called kinase inhibitors, specifically a second-generation irreversible inhibitor of the ErbB family. Certain cancer cells rely on abnormal epidermal growth factor receptor (EGFR) proteins to send continuous growth and survival signals, allowing the tumour to grow and spread. Afatinib irreversibly binds to and blocks the entire ErbB receptor family, shutting down these signaling pathways to slow or stop cancer cell growth. It comes as a film-coated tablet taken by mouth. This medicine treats adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have specific genetic mutations in the EGFR gene, or patients with metastatic squamous NSCLC that has progressed after platinum-based chemotherapy. Before starting treatment for non-small cell lung cancer, a validated test must confirm an EGFR mutation. Afatinib is an oral medicine taken once daily at home on an empty stomach. Treatment is started and supervised by a specialist doctor, and it continues as long as the cancer keeps responding and side effects remain manageable.

Uses

Afatinib is used to manage adults with advanced or metastatic non-small cell lung cancer that carries specific abnormal epidermal growth factor receptor (EGFR) mutations.

Contraindications

When should one not use Afatinib

If you are allergic to Afatinib.

Side effects

Common side effects of this drug are:

Diarrhoea ( sometimes severe)
Skin rash, acne-like bumps, and itchy skin
Mouth sores and ulcers
Inflammation of the skin around the nails (paronychia)
Decreased appetite and weight loss
Nausea and vomiting
Dry skin
Fatigue and weaknessChanges in taste (dysgeusia)
Nosebleeds
Dry eyes, watery eyes, or eye irritation (conjunctivitis)
Indigestion or heartburn
Lip inflammation or chapping (cheilitis)
Elevated liver enzymes in blood tests
Fever (pyrexia)Severe diarrhoea: causes excessive fluid loss (dehydration) and severe kidney complications.
Serious lung inflammation (interstitial lung disease/pneumonitis): It can be severe, life-threatening, or fatal; symptoms include new or worsening shortness of breath, cough, fever, or chest pain.
Severe skin reactions: Severe blistering, peeling skin, or painful spreading rash.
Serious liver problems: Symptoms include yellowing of the skin or eyes (jaundice), dark urine, and upper right abdominal pain.
Stomach or intestinal perforation: Symptoms include sudden, severe stomach pain or black/tarry stools.
Serious eye problems: Report eye pain, severe redness, blurred vision, or other new vision problems promptly.

Precautions and Warnings

Pregnancy

Afatinib should not be used during pregnancy unless your doctor considers it essential, as it may harm an unborn baby. Use effective contraception during treatment and for the period your doctor advises afterwards.

Breast Feeding

Breastfeeding is not recommended during treatment with afatinib because it is likely to pass into breast milk and may harm the infant.

Driving

Afatinib can cause side effects like severe tiredness (fatigue) or eye problems (such as redness, dry eyes, or watery eyes) that may impair your ability to drive safely. If you experience fatigue, feel unwell, or notice changes in your vision, avoid driving or operating machinery and consult your doctor.

Alcohol

There is no specific established alcohol interaction with afatinib. However, alcohol may worsen symptoms such as diarrhoea, nausea, fatigue, or dehydration. Ask your doctor whether alcohol is appropriate for you.

Other General Warnings

Talk to your doctor if

You experience frequent or severe diarrhoea, as it can cause fluid loss and lead to kidney issues if not managed properly.
You develop severe skin reactions, a widespread rash, severe itching, or blistering.
You experience sudden or worsening shortness of breath, a persistent cough, or fever, as these may signal serious lung inflammation.
You have heart problems, as left ventricular dysfunction has been reported, and your doctor may consider cardiac monitoring when appropriate.
You have liver problems, so your doctor may need to monitor liver function.
You notice severe eye redness, eye pain, blurred vision, or excessive tears.

Mode of Action

How Does It Work?

Afatinib works by blocking proteins in the ErbB receptor family, including EGFR (ErbB1), HER2 (ErbB2), ErbB3 and ErbB4. These proteins can signal to promote cancer-cell growth and spread. Afatinib binds irreversibly to these receptors and blocks their signalling, helping to slow the growth and spread of cancer cells.

Interactions

Interactions with other medicines

Some medicines can affect the amount of afatinib in your body. Tell your doctor about all medicines, supplements, vitamins, and herbal products you take.
Important interactions include:
Medicines used to treat heart problems or high blood pressure (such as verapamil or quinidine)
Antifungal medicines (such as ketoconazole or itraconazole)
Antibiotics used for bacterial infections (such as erythromycin or rifampicin)
Medicines for fits or brain-related disorders (such as carbamazepine or phenytoin)
Herbal remedies like St. John's Wort
Medicines used to manage stomach acid or indigestion

Interactions with food items

Afatinib must always be taken on an empty stomach. Food in the stomach reduces how much medicine your body absorbs, which can lower its effectiveness. Do not eat anything for 2 hours before taking your tablet, and wait at least 1 hour after taking it before eating.

Dosage

Overdose

If an overdose is suspected, stop the medicine and contact your doctor immediately or visit the nearest emergency department for appropriate supportive care.

Missed a Dose

If you miss a dose, take it as soon as you remember unless your next dose is due within 12 hours. If it is within 12 hours, skip the missed dose and take your next dose at the usual time. Do not take two doses together. Always consult the doctor before taking the missed dose.

Frequently Asked Questions (FAQs)

EGFR is a protein involved in cell growth. Certain changes, or mutations, in the EGFR gene make cancer cells receive constant growth signals. Afatinib blocks signalling through the ErbB family, including EGFR, which slows the growth and spread of those cells. A laboratory test confirms the mutation before treatment starts.

Food reduces how much of the medicine the body absorbs, which can make the treatment less effective. Take it well before or well after food, as directed by your doctor.

Diarrhoea is one of the most common effects. Drink extra fluids to prevent dehydration and contact your doctor, who will usually prescribe an anti-diarrhoeal medicine and advise you on managing it.

Treatment continues for as long as the cancer responds and the side effects remain manageable. Your doctor will review you regularly with examinations and scans.