Description

Azarest tablet: Each film coated tablet contains Azacitidine INN 300 mg.

 

Product Features

Product Name	:	Azarest
Generic Name	:	Azacitidine
Formulation	:	Tablet
Available Pack Size	:	14’s Pot
Available Strength	:	300 mg
Registrations	:	Export Only

Indication

Azarest (Azacitidine) is used to keep treating adult patients with acute myeloid leukemia who:

• Reached first complete remission (CR) or complete remission with incomplete blood count recovery (CRi) after intense initial chemotherapy.
• Can’t finish intense curative therapy.

 

Azacitidine mechanism of action

Azacitidine drug works like a mimic of cytidine, a building block of DNA and RNA. It stops certain enzymes in the body from adding methyl groups to DNA and RNA. When cells take in Azarest and transform it with enzymes, it becomes part of the DNA and RNA molecules. This incorporation into DNA of cancer cells, like those in acute myeloid leukemia, blocks the action of DNA methyltransferases.

 

This leads to less DNA methylation and changes how genes work. Some genes that help control tumors and cell development start working again. When Azacitidine becomes part of RNA in cancer cells, it also blocks the action of RNA methyltransferases. This leads to less RNA methylation, making RNA less stable and reducing protein production.

 

In lab studies, Azacitidine added to the DNA of cancer cells, especially those in acute myeloid leukemia, caused cell death and made cells self-destruct. This effect was also seen in living animals with leukemia tumors treated with Azarest. It reduced tumor size and helped the animals live longer.

 

Absorption

When you take Azacitidine by mouth, about 11% of it ends up in your bloodstream compared to when it’s given under the skin. It takes around 1 hour for Azacitidine to reach its highest level in the blood after you take it.

 

Dosage and Administration

Don’t switch Azacitidine with the intravenous or subcutaneous forms. The reasons you take them and how much you take are different.

For the first 14 days of a 28-day cycle, take 300 mg of azacitidine orally every day. It can be taken with or without meals. Continue using azacitidine unless you notice serious side effects or your illness worsens. Take an anti-nausea medication half an hour before each dose during the first two cycles. You can forgo taking the anti-nausea medication in subsequent cycles if you haven’t experienced nausea or vomiting during the first two.

Avoid taking Azacitidine if your blood test results on Day 1 of a cycle indicate a low absolute neutrophil count (ANC) of less than 0.5 Gi/L. To begin the cycle, wait until your ANC is 0.5 Gi/L or greater.

 

Instruction to follow

Patients should be advised not to split, crush, or chew Azacitidine tablets. Take a dose every day at roughly the same time. Azarest should be taken as soon as possible on the same day if it is missed or not taken at the scheduled time. Then, follow your regular routine the next day.

Avoid taking two doses on the same day; if a dose causes vomiting, avoid taking another one on the same day. Go back to your regular schedule the next day. Azacitidine is a medication with risks. Observe the relevant special handling and disposal guidelines.

 

Azacitidine side effects

Clinical Trials Experience

• Serious Reactions: About 15% of patients had serious side effects, such as pneumonia and febrile neutropenia (low white blood cell count with fever). One patient died due to sepsis.
• Discontinuation: 8% stopped taking Azarest because of side effects like nausea, diarrhea, and vomiting.
• Interruptions: 35% had to pause treatment due to side effects, mainly neutropenia (low white blood cell count), thrombocytopenia (low platelet count), and nausea.
• Dose Reductions: 14% had their dose reduced because of side effects, mainly for neutropenia, diarrhea, thrombocytopenia, and nausea.
• Common Side Effects: Nausea, vomiting, diarrhea, fatigue, constipation, pneumonia, abdominal pain, joint pain, decreased appetite, febrile neutropenia, dizziness, and limb pain were the most frequent side effects, each affecting over 10% of patients.

Post-marketing Experience

Some adverse reactions reported after approval include hypersensitivity reactions, lung problems, tumor lysis syndrome, Sweet’s syndrome (a skin condition), necrotizing fasciitis (serious skin infection), and differentiation syndrome.