Olaparib drug

Indications

Olaparib is indicated to treat breast cancer, ovarian cancer, fallopian tube cancer, peritoneal cancer, pancreatic cancer, and prostate cancer. Olaparib is a medication classified as a PARP inhibitor. PARP stands for poly(ADP-ribose) polymerase, which is an enzyme involved in DNA repair. 

 

Olaparib works by inhibiting this enzyme, leading to the accumulation of DNA damage in cancer cells. This makes it particularly effective in cancers with certain genetic mutations, such as BRCA1 or BRCA2 mutations, which impair the cell’s ability to repair DNA damage.

 

Olaparib FDA Approval

KuDOS Pharmaceuticals, a UK-based biotechnology company founded by Stephen Jackson of Cambridge University, first administered olaparib to patients. Olaparib received approval from the US Food and Drug Administration (FDA) and the European Medicines Agency (EMA) as monotherapy in December 2014.

 

The FDA specifically approved olaparib for advanced ovarian cancer with germline BRCA mutations (gBRCAm) that had undergone three or more prior lines of chemotherapy. 

 

In January 2018, olaparib made history as the first PARP inhibitor to gain FDA approval for gBRCAm metastatic breast cancer.

 

Subsequently, in August 2017, olaparib tablets received US approval for maintenance treatment in adults with recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer, provided they had achieved either complete or partial response to platinum-based chemotherapy. 

Olaparib capsules and tablets are not interchangeable.

 

Mechanism of Action

Understanding DNA Repair: Our cells have mechanisms to repair damaged DNA. Think of DNA as the instruction manual for our cells. Sometimes, due to various reasons like exposure to radiation or chemicals, our DNA gets damaged.

 

Role of PARP Proteins: Inside our cells, there’s a protein called PARP (Poly ADP-Ribose Polymerase). PARP helps in repairing damaged DNA. When there’s a nick or a break in the DNA, PARP jumps into action, like a repair crew fixing a tear in a piece of paper.

 

Exploiting Vulnerabilities: Now, here’s where olaparib comes in. Olaparib is a type of drug called a PARP inhibitor. It’s like a special tool that blocks the PARP protein from doing its job. So, when cancer cells, which already have some DNA damage, can’t use PARP to fix that damage, they become even more vulnerable.

 

Leading to Cell Death: With PARP blocked by olaparib, cancer cells can’t repair their DNA properly. This leads to a buildup of damage in the cancer cells. Eventually, they can’t survive and start to die off.

 

So, in simple terms, olaparib works by blocking a protein called PARP, which cancer cells rely on heavily for DNA repair. By doing so, it helps prevent cancer cells from fixing their damaged DNA, ultimately leading to their demise.

 

Olaparib Side Effects

Some common side effects of olaparib may include nausea, fatigue, vomiting, diarrhea, loss of appetite, and headache. Additionally, olaparib can cause certain blood disorders such as anemia, low platelet count (thrombocytopenia), and low white blood cell count (neutropenia), which may increase the risk of infection or bleeding. Some people may also experience changes in their liver function tests or develop lung problems like cough or shortness of breath. 

 

It’s important to note that these side effects can vary in severity from person to person.

 

Dosages And Administration

For the treatment of advanced ovarian cancer, the recommended dosage of olaparib tablets is typically 300 mg (two 150 mg) taken orally twice daily. This dosage may be adjusted based on individual patient tolerability and response to treatment.

 

For the treatment of metastatic breast cancer with germline BRCA mutations, the recommended dosage of olaparib tablets is also typically 300 mg (two 150 mg) taken orally twice daily.

 

In the case of maintenance treatment for recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer, the recommended dosage of olaparib tablets is typically 300 mg taken orally twice daily as well.

 

How to take Olaparib?

Olaparib tablets should be swallowed whole with water and can be taken with or without food. Patients should not chew, crush, or break the tablets before swallowing.

 

Missed a Dose?

If a dose of olaparib is missed, patients should not take an extra dose to make up for it but should continue with their regular dosing schedule.