Microplastics and Misinformation: What Science Really Says
November 12, 2025
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Brand Name :
Tarceva
(United States) [Available]Synonyms :
Erlotinib
Class :
Antineoplastics and Tyrosine Kinase Inhibitor
Brand Name :
Tarceva
(United States) [Available]Synonyms :
Erlotinib
Class :
Antineoplastics and Tyrosine Kinase Inhibitor
Dosage Forms & Strengths  Â
Tablet  Â
25mg  Â
100mg  Â
150mg  Â
150
mg
orally
once a day
;before 1 hour or 2 hours after meals
the duration of the therapy continues until disease progression, or unacceptable toxicity occurs
It is used for the patients with metastatic non-small cell lung cancer and for the tumors which have epidermal growth factor receptor exon 19 deletions or exon 21 substitution mutations receiving first-line maintenance or second-line treatment after progression following at least one prior chemotherapy regimen
100
mg
Orally
once a day
; before 1 hour or 2 hours after meals
the duration of the therapy continues until disease progression, or unacceptable toxicity occurs
It is used for patients in combination with gemcitabine as a first-line treatment for patients with locally advanced, unresectable, or metastatic pancreatic cancer
Dose Adjustments
Renal Dose Adjustments:
for renal impairment, dosage adjustment requires, and caution is recommended.
Liver Dose Adjustments:
The treatment should be discontinued in patients with baseline hepatic impairment if the total serum bilirubin doubles or serum transaminases triple
The treatment should be discontinued in patients with normal pretreatment values if the total serum bilirubin >3 x ULN or serum transaminases >5 x ULN
when both drugs are combined, there may be a decrease in levels of serum concentration and absorption of erlotinib  
when both drugs are combined, there may be a decrease in levels of serum concentration and absorption of erlotinib  
when both drugs are combined, there may be a decrease in levels of serum concentration and absorption of erlotinib  
when both drugs are combined, there may be a decrease in levels of serum concentration and absorption of erlotinib  
when both drugs are combined, there may be a decrease in levels of serum concentration and absorption of erlotinib  
when both drugs are combined, there may be a decrease in levels of serum concentration and absorption of erlotinib  
erlotinib: they may diminish the serum concentration of CYP3A4 inducers
erlotinib: they may diminish the serum concentration of CYP3A4 inducers
erlotinib: they may diminish the serum concentration of CYP3A4 inducers
erlotinib: they may diminish the serum concentration of CYP3A4 inducers
erlotinib: they may diminish the serum concentration of CYP3A4 inducers
erlotinib: they may diminish the serum concentration of antacids
erlotinib: they may diminish the serum concentration of antacids
erlotinib: they may diminish the serum concentration of antacids
erlotinib: they may diminish the serum concentration of antacids
erlotinib: they may diminish the serum concentration of antacids
erlotinib: they may diminish the serum concentration of antacids
when both drugs are combined, there may be an increased level of serum concentration of erlotinib  
when both drugs are combined, there may be an increased metabolism of erlotinib  
when both drugs are combined, there may be an increased metabolism of erlotinib  
when both drugs are combined, there may be a reduced metabolism of erlotinib  
when both drugs are combined, there may be a reduced metabolism of erlotinib  
when both drugs are combined, there may be an increased risk or severity of adverse effects    
when both drugs are combined, there may be a reduced metabolism of idelalisib  
when both drugs are combined, there may be a reduced metabolism of erlotinib  
when both drugs are combined, there may be a decreased level of serum concentration of erlotinib  
when both drugs are combined, there may be a reduced metabolism of erlotinib  
when both drugs are combined, there may be a reduced metabolism of erlotinib  
when both drugs are combined, there may be a reduced metabolism of erlotinib  
when both drugs are combined, there may be a reduced metabolism of erlotinib  
when both drugs are combined, there may be a reduced metabolism of tucatinib    
the effect of erlotinib is decreased by lorlatinib, by altering intestinal or hepatic CYP3A4 enzyme metabolism
CYP3A strong enhancers of the small intestine may reduce the bioavailability of erlotinib
when both drugs are combined, there may be a reduced metabolism of erlotinib  
when both drugs are combined, there may be a decreased level of serum concentration of erlotinib  
when both drugs are combined, there may be a reduced metabolism of erlotinib  
when both drugs are combined, there may be a decreased metabolism of atorvastatin  
when both drugs are combined, there may be a decreased level of serum concentration of erlotinib  
when both drugs are combined, there may be a decreased level of serum concentration of erlotinib  
when both drugs are combined, there may be a decreased level of serum concentration of erlotinib  
when both drugs are combined, there may be a decreased effect of erlotinib by increasing hepatic clearance  
when both drugs are combined, there may be a decrease in levels of serum concentration and absorption of erlotinib  
when both drugs are combined, there may be an increased level of serum concentration of erlotinib  
when both drugs are combined, there may be a decreased level of serum concentration of erlotinib  
when both drugs are combined, there may be a reduced metabolism of erlotinib  
when both drugs are combined, there may be an increased metabolism of erlotinib  
when both drugs are combined, there may be an increased metabolism of erlotinib  
when both drugs are combined, there may be a reduced metabolism of erlotinib  
when both drugs are combined, there may be a reduced metabolism of erlotinib  
when both drugs are combined, there may be a reduced metabolism of erlotinib 
It may diminish the effect when combined with griseofulvin by CYP3A4 metabolism
when bromazepam and erlotinib are used together, there is a potential reduction in the bromazepam's metabolism
When erlotinib is used together with somatotropin, this leads to a rise in erlotinib metabolism
When erlotinib is used together with adenosine, this leads to enhanced risk or seriousness of QTc prolongation
When erlotinib is used together with ridaforolimus, this leads to enhanced concentration serum of erlotinib
nafcillin will decrease the effect of action of erlotinib by affecting enzyme CYP3A4 metabolism
lapatinib increases the effect of erlotinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
encorafenib increases the toxicity of erlotinib and decreases its effectiveness by altering intestinal/hepatic CYP3A4 enzyme metabolism
fedratinib increases the effect of erlotinib by altering the intestinal/ hepatic CYP3A4 enzyme metabolism
may enhance the serum concentration of CYP3A4 Inhibitors
the risk of QTc prolongation may be increased
When erlotinib is aided by hesperetin, it reduces hesperetin’s metabolism
Erlotinib is a reversible first-generation tyrosine kinase inhibitor that primarily targets the epidermal growth factor receptor (EGFR), a member of the ErbB receptor family. It binds to both the normal (wild-type) and mutated forms of EGFR. EGFR and related ErbB receptors can form dimers that activate signaling pathways involved in cancer development, such as cell differentiation, proliferation, and angiogenesis. By inhibiting EGFR phosphorylation, erlotinib disrupts these pathways, helping to control tumor growth. Activating EGFR mutations, often found in non-small cell lung cancer (NSCLC), are more common in non-smokers, females, individuals of Asian descent, and those with adenocarcinoma. Additionally, erlotinib affects liver enzymes by inducing CYP1A1 and CYP1A2 and moderately inhibiting CYP3A4 and CYP2C8, which can influence drug metabolism.Â
Adverse drug reactions: Â
Frequency defined Â
>10% Â
Increased creatinine Â
Decreased white blood cell count Â
decreased neutrophil count Â
anemia Â
decreased lymphocyte count Â
decreased platelet count Â
neutropenia Â
Leukopenia Â
Thrombocytopenia Â
Diarrhea Â
nausea Â
abdominal pain Â
vomiting Â
constipation Â
stomatitis Â
dry mouth   Â
Fatigue Â
infections Â
peripheral edema Â
Pyrexia Â
1-10% Â
Interstitial lung disease Â
Pneumonitis Â
Arthralgia Â
Venous thromboembolic events Â
 Â
There is no FDA-mandated black box warning specifically for erlotinibÂ
ContraindicationsÂ
Known hypersensitivity to erlotinib or any of its components.Â
CautionsÂ
Risk of potentially fatal interstitial lung disease (ILD); stop if symptoms like new/worsening cough, dyspnea, or fever occur.Â
Increased risk of myocardial infarction, cerebrovascular accident, and microangiopathic hemolytic anemia in pancreatic cancer patients.Â
No benefit after disease progression.Â
Avoid pregnancy due to fetal risk; use effective contraception during and 1 month after treatment.Â
Eye issues (dryness, abnormal eyelash growth, keratitis) may lead to serious corneal damage; discontinue if acute eye problems develop.Â
Pregnancy warnings:   Â
Breastfeeding warnings:Â
Pregnancy Categories:     Â
Erlotinib competitively inhibits the tyrosine kinase domain of EGFR by binding to the ATP-binding site, thereby blocking autophosphorylation and downstream signaling pathways involved in cell proliferation and survival. It is metabolized primarily by CYP3A4 in the liver and has a half-life of approximately 36 hours. Its inhibition of EGFR is dose-dependent and correlates with antitumor activity.Â
PharmacokineticsÂ
AbsorptionÂ
Erlotinib has an oral bioavailability of approximately 60%, which can increase to nearly 100% when taken with food. It reaches peak plasma concentration around 4 hours after administration.Â
The half-life of erlotinib is about 36 hours.Â
DistributionÂ
Erlotinib is highly protein-bound, with 93% binding in plasma.Â
MetabolismÂ
It is primarily metabolized by the liver enzyme CYP3A4, with minor contributions from CYP1A2 and the extrahepatic enzyme CYP1A1.Â
Elimination/ExcretionÂ
The drug is mainly excreted via feces (83%), with a smaller portion eliminated in urine (8%).Â
PharmacodynamicsÂ
Erlotinib works by selectively inhibiting the tyrosine kinase activity of the epidermal growth factor receptor (EGFR), a protein involved in cell signaling pathways that regulate cell growth and division. By blocking EGFR, erlotinib disrupts these signals, leading to the inhibition of tumor cell proliferation and inducing cancer cell death. This mechanism is particularly effective in cancers with activating EGFR mutations, where the receptor is overactive.Â
Erlotinib is available as oral tablets in 25 mg, 100 mg, and 150 mg strengths. For NSCLC, erlotinib’s starting dose is 150 mg daily, while for pancreatic cancer combined with gemcitabine, it’s 100 mg daily. ASCO guidelines recommend gemcitabine alone for metastatic pancreatic cancer patients with poor performance or comorbidities, adding erlotinib cautiously with dose adjustments. Erlotinib should be taken on an empty stomach due to its narrow therapeutic index and increased bioavailability with food.Â
Generic Name: ErlotinibÂ
Pronunciation: er-LOH-ti-nibÂ
Erlotinib treats pancreatic and lung cancer by retarding or stopping the growth of cancer cells.
The medication is taken orally, empty stomach before 1 hour and after 2 hours of the meals.
Be sure to inform your physician about your previous medications or allergy to any substance.
Antacids or H2 blockers may prevent the erlotinib from getting completely bioavailable.
Do not variate the dose by yourself; ask your doctor to do it.
Erlotinib’s side effects include dry skin, diarrhea, mouth ulcers, muscular pain, extensive eyelash growth, nausea, vomiting, loss of appetite, abdominal pain, and dehydration.
If any of the side effects get worsen, immediately consult your doctor.
Never share your medication with anyone.
Keep on getting your kidney, and other vital organs checked regularly during the treatment period.
Store the medicine in a cool and moisture-free place.
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