Erlonat (Erlotinib), (A metastatic Non-small cell lung cancer drug)Abstract:
Erlonat (Erlotinib), it is a hydrochloride salt of quinazoline derivative with anti-tumor activity.
Erlonat exhibits its activity by binding to intracellular catalytic region of EGFR (epidermal growth factor receptor) tyrosine kinase.
Therefore signal transduction will be inhibited and leads to cell death.
Erlonat involved in cell lysis by inhibiting the signal transduction of cancer cells through epidermal growth factor receptors, which are present on the surface of the cancer cells and also in normal cells.
Tyrosine kinase inhibitors proceed its action on EGFR which may leads to block angiogenesis and cellular multiplication (cell division).
Erlonat is primarily used for the treatment of;
Advance or metastatic non small cell lung cancer.
Pancreatic cancer by combining with gemcitabine.
Pregnancy and women who become pregnant
Drug name: Erlotinib
Type of drug: Tyrosine kinase inhibitor or Anti-neoplastic agent
Used for: metastatic non-small cell lung cancer & pancreatic cancer
Also known as: Erlonat
Available strength: 150MG
The pregnancy category of Tablet erlonat comes under “D”
Erlonat should not be recommended in pregnancy and lactation period.
Erlonat cause harm to the unborn babies
The storage condition of Erlonat tablets container should be kept at 25oC (77oF); excursion between 15oC to 30oC
Container should be keep away from moisture, heat and light.
Interstitial lung disease
Bullous and exfoliative skin disorders
Embryo fetal toxicity
60% of drug absorbed after oral administration; the peak plasma concentration of the drug occurs within 4 hours The bioavailability of the drug 60% but increased by food to 100%
Nearly 93% of drug bound to the human plasma protein.
Most of the drug metabolized in liver with the help of cytochrome isoenzymes like CYP3A4 to lesser extent CYP1A4.
The elimination routes are feces and urine. The half life is around 36 hours.
Avoid concomitant with proton pump inhibitors. Erlonat should be administered 10 hours after the H2 receptor antagonist and at least 2 hours before the next dose of H2 receptor antagonist.
In case of missed dose, the patient should be advice by taking missed tablet within the period of next dose; otherwise the dose will be skipped and follow the regular dosing schedule. Do not double the dose
Avoid these concomitants (combinations)
Aprepitant: increase the serum concentration of CYP3A4 substrates
Bosentan: depletes the serum concentration of CYP3A4 substrates
Ceritinib: increase the serum concentration of CYP3A4 substrates
Ciprofloxacin: elevate the serum concentration of Erlotinib
Conivaptan: increase the serum concentration of CYP3A4 substrates
CYP3A4 inducers (moderate or strong) decrease the serum concentration of Erlotinib and CYP3A4 inhibitors (moderate and strong) decrease the metabolism and increase the serum concentration respectively
Dabrafenib, dasatinib, deferasirox, Enzalutamide, proton pump inhibitors, H2 receptor antagonist etc
Cardiovascular: chest pain, peripheral edema
Central nervous system: fatigue, headache, dizziness, insomnia, paresthesia,
Dermatologic: skin rash, Pruritus, paronychia, alopecia, acne, vulgaris
GIT: diarrhea, anorexia, nausea, loss of appetite, vomiting, stomatitis, abdominal pain
Genitourinary: urinary tract infection
Muscle: weakness, back pain, arthralgia, musculoskeletal pain
Ophthalmic: conjunctivitis, keratoconjuctivitis sicca
Pulmonary: cough, dyspnea
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