NUBLEXA 40 MG

Description

Nublexa 40mg is a cancer medicine whichinhibits the growth and spread of cancer cells in the body.

Nublexa 40mg is usually administer after other cancer medications have been tried without success.

Nublexa 40mg is a prescription drugs which is used under the supervision of medical practioners.

Indication

Nublexa 40mg is indicated for the treatment following conditions

Hepatocellular carcinoma

Colorectal cancer

Gastrointestinal stromal tumor

Dosage and administration

Hepatocellular carcinoma

The prescribed dose is 160mg (four 40mg tablets) Po q Day for the first 21 days of each 28-day cycle.

Follow the treatment of this conditions until disease progression or undesirable toxicity

Colorectal cancer

The usual dose is 160mg (four 40mg tablets) Po q Day for the first 21 days of each 28-day cycle.

Gastrointestinal stromal tumor

The usual dose is 160mg (four 40mg tablets) Po q Day for the first 21 days of each 28-day cycle.

Mechanism of action

Regorafenib belongs to targeted cancer drug. It works by preventing proteins on cancer cells which encourages the cancer to develop. These proteins are called protein kinases. Therefore, regorafenib is called a protein kinase inhibitor (TKI) or cancer growth blocker. 

It also inhibits the cancer cells from growing blood vessels which they required. Preventing blood vessel growth is called anti-angiogenesis treatment. 

Regorafenib may decrease the cancer or stops it growing for a time.  

ADME Properties

Time to peak plasma is 4 hours and concentration is 2.5mcg/mL for single dose; 3.9mcg/mL for steady state and bioavailability is 69-83%

Regorafenib has protein bounding about 99.5% and M-2 active metabolite is 99.8%; M-5 active metabolite is 99.95%

Regorafenib is metabolized by CYP3A4 and UGT1A9

Excreted via feces 71%; 19% urine (within 12 days of single dose)

Half-life of

Regorafenib is 28 hr

M-2 active metabolite is 25 hr

M-5 active metabolite is 51hr

Side effects

Common side effects occurring in greater than 30%

• High bilirubin in the blood
• Hand-foot syndrome
• Diarrhea
• Low platelets
• Mouth sores/inflammation
• Weight loss
• Infection
• Anemia
• Increased liver enzymes (AST, ALT)
• Fatigue
• High blood pressure
• Protein in the urine
• Low calcium
• Low phosphorous
• Low white blood cells
• Decreased appetite
• Increased lipase& amylase
• Voice disorder (Dysphonia)
• Low sodium
• Nausea

Less common side effects occurring in about 10-29% of patients receiving Nublexa 40mg

• Increased bleeding
• Headache
• Alopecia
• Pain
• Fever
• Rash
• Low potassium
• Decreased blood clotting

Drug interaction

Interaction of Nublexa 40mg with strong CYP3A4 inducers will decrease Regorafenib plasma concentrations and increased plasma concentration of active metabolite M-2; M-5.

Interaction of Nublexa 40mg with strong CYP3A4 inhibitor will increase Regorafenib plasma concentration and decreased plasma concentration of active metabolite M-2; M-5.

Interaction of Nublexa 40mg with BCRP substrate will increased the plasma concentration of the BCRP substrate.

Precautions

• While therapy with Nublexa will have high risk for HFSR/PPES and rash; a more incidence of HFSR reported in Asian patients; stop and then reduce or stop regorafenib depending on severity and persistence of dermatologic toxicity
• When administrating Nublexa 40mg will occur Myocardial ischemia and infarction seen in clinical trials; withhold Nublexa for new or acute cardiac ischemia/infarction and restart only after resolution of acute ischemic events
• While therapy with Nublexa, one case report of reversible posterior leukoencephalopathy syndrome (RPLS) occurred (1 of 1100 treated patients); discontinue therapy if RPLS occurs
• Severe drug-induced liver injury with fatal outcome appeared in Nublexa-treated patients in clinical trials. Some of the cases, liver dysfunction occurred within the first 2 months of treatment and was characterized by a hepatocellular pattern of injury.
• While treatment with Nublexa will have heavy risk for haemorrhage; stop therapy for severe or life-threatening haemorrhage
• While therapy with Nublexa will Increased risk of infections reported; most common infections includes urinary tract infections, nasopharyngitis, mucocutaneous and systemic fungal infections and pneumonia

Pregnancy

There are no data available on use in pregnant women. Advise female about the possible hazard to a foetus.

Lactation

Excretion into human milk is unknown

Avoid breast feeding during the treatment with Nublexa 40mg

Storage

Store the Nublexa 40mg at 25⁰C (77⁰C)

Keep the drug in its original container bottle

Keep the bottle tightly closed after one time used

Missed dose

If dose is missed, patients must consult with medical practitioner and follow the instructions given by them.

thereby missed dose should be avoid and follow the regular dosing schedule