Herduo 250mg

Herduo 250mg tablets are classified as an anti-cancer agent, which is orally active drug used for treating breast cancer.

Chemically classified as quinazoline with strong anti-cancer effect and the tablet Herduo is a synthetic oral tablet.

Normally targeted therapy or tyrosine kinase inhibitor drugs can increase the plasma aminotransferase levels which may lead to liver injury.

Herduo 250mg tablets are classified as;

1.Tyrosine kinase prohibition

2.Stop the HER2/neu& epidermal growth factor receptor activity

3.Targeted therapy

4.Signal transduction prohibition.

INDICATION

Primarily Herduo 250mg tablet indicated for advanced breast cancer. Herduo 250mg is indicated for the combination with Capecitabine tablets are normally indicated for the treatment of metastatic breast cancer patients in whose cancer cells expressed with EGFR 2 (HER2) and already patients may get an anthracycline, taxane & Trastuzumab.

herduo 250mg,herduo 250mg tablet

DOSAGE

In HER2 positive advanced breast cancer:

The usual dose of Herduo 250mg is 1250mg should be given orally as a single dose on day 1 to 21 repeatedly concomitant with Capecitabine 2000mg/m2/day (administer 2 doses relatively 12 hours apart orally) on day 1 to 14 in a continuous 21-day cycle.

Sum of 5 tablets of Herduo should be given at a time as a whole.

Patients with hormone receptor-positive HER 2 positive advanced breast cancer:

The usual dose is 1500mg should be given orally as a single dose by combination with letrozole.

The usual dose of letrozole is 2.5mg as a once daily

Administer 6 tablets of Herduo 250mg in this condition

Dose alteration:

Cardiac events:

Left ventricular ejection fraction with grade 2 reduction in patients is given treatment with Herduo should be discontinued. In this condition, the dose of Herduo should be started with 1000mg/day in combining with Capecitabine; whereas in combination with letrozole the dose of Herduo restated with 1250mg/day after 2 weeks, if LVEF turns to normal. Hepatic impairment:

Severe hepatic impairment in patients, the dose reduced from 1250mg/day to 750mg/day or from 1500mg/day to 1000mg/day. Administer the Herduo tablet without food as 1 hour before or 2 hours after the uptake of food.

PHARMACOLOGY

Chemically Herduo is classified as 4-anilinoquinazoline derivative, that evacuates anti-cancer activity by inhibiting intracellular tyrosine kinase domains of EFGR & HER type 2.

The ErbB forced cancer cell production has been prevented by Lapatinib.

This growth factor receptor present on the cell surface of cancer mass which may lead to cause cell death.

Absorption:

Incomplete and insufficient absorption, the time to peak plasma concentration is 4 hours after intake of the drug.

Distribution :

The drug bounds to human plasma protein like albumin & alpha glycoprotein relatively 99%.

Metabolism :

Herduo 250mg tablet is a substrate of P-gp& BCRP and go through intensive metabolism by using CYPP3A4 & CYP3A5 with a minimum contribution of CYP2C19 & CYP2C8.

Excretion :

Elimination occurs via feces & urine.

Half-life time in 14.2 hours reaches by a single dose of Herduo 250mg and multiple dosing reaches in 24 hours

PRECAUTION

Reduction in left ventricular ejection fraction:

While using Herduo in a patient with LVEF Caution should be taken

The resentment of LVEF should be decreased within the first 12 weeks of treatment

Before starting the therapy with Herduon 250mg, the patient must be monitor thoroughly if suspected with LVEF or not.

Liver damage: 

Raising the level of AST, ALT or bilirubin may cause liver injury

To inhibits this condition, periodic LFT should be control

Diarrhea:

Serious diarrhea may cause to dehydration leads death also; if the patient does not recover from this severity must stop with this therapy.

Interstitial lung disease:

The patient should be check with pulmonary symptoms and give supportive measures.

On Serious condition, treatment should be discontinuing

QT prolongation:

Balance ECG periodically

Give the patient substituent for this adverse condition

Hypokalemia and hypomagnesemia correction should take place

Cutaneous reactions: 

Some life-threatening reactions may occur, in this condition, therapy should be discontinued

Embryo-fetal damage:

Herduo 250mg leads to fetal damage and produce some deformities.

During therapy Patient should advice not getting pregnant.

DRUG INTERACTION

The drug Herduo are the prohibition of CYP3A4, CYP2C8 & P-gp drug transporters; a weak inhibitor of CYP3A4.

Interaction of Midazolam withHerduo 250mg, increases the exposure of Midazolam

Interaction of Paclitaxel Will Increase in paclitaxel exposure occurs while concomitant with Herduo 250mg tablet.

Digoxin interaction with Herduo 250mg then the Serum digoxin concentration should be examined periodically prior to starting the concomitant use.

A drug that induces or inhibit CYP3A4 enzymes:

If the interaction of Herduo tablets with CYP3A4 inducers or inhibitors, alteration of the dose is necessary.

Interaction of Ketoconazole with Herduo 250mg, the dose reduced to 200mg as two times a day for 7 days.

Interaction of Carbamazepine with Herduo 250mg tablet, the dose of carbamazepine at 100mg as two times a day for 3 days & 200mg for two times a day for 17 days, the exposure of Herduo reduced to 72%.

Concomitant use of Herduo 250mg with P-gp inhibitors causes increasing the concentration of Lapatinib.

CONTRAINDICATION

The patients who are contraindicated to the component present in Herduo 250mg tablet then Hypersensitivity reaction occurs.