PARP Inhibitors 2017

Poly (ADP-ribose) polymerase (PARP) inhibitors are targeted therapies that are used for multiple indications, most commonly, cancer. PARP aids in cellular growth, regulation and repair of cells.The PARP inhibitor stops the cancer cells being repaired which causes the cells to die thus reducing the tumor growth. Numerous cancer forms are more dependent on PARP than regular cells, making it an attractive target for cancer therapy. Currently they are used to treat ovarian cancer, fallopian tube cancer and peritoneal cancer. These inhibitors are considered as a potential treatment for acute life-threatening diseases, such as stroke and myocardial infarction, along with neurodegenerative diseases. Currently this class of drug is becoming popular which can be deduced from the increased research as seen in the below clinical trial data from past few years.

Clinical Trials

2017 (Till Sep)

2016

2015

2014

2013

Early Phase 1

1

1

1

0

0

Phase 1

9

11

9

7

3

Phase 2

13

14

11

7

3

Phase 3

2

3

3

2

7

Total

25

29

24

16

13

Growth YoY

21%

50%

23%

30%

There have been around 173 studies on PARP inhibitors with 55 completed studies and 3 studies with results. Olaparib, Niraparib and Rucaparib are the commercially available PARP inhibitors.

Olaparib:

This is commercially available as Lynparza, produced by AstraZeneca, Inc., (earlier, KuDOS Pharmaceuticals). It is used to treat ovarian cancer, fallopian tube cancer, or peritoneal cancer. It is a monotherapy used in patients with deleterious or suspected deleterious germline BRCA mutated advanced cancer who have been treated with three or more prior lines of chemotherapy. Olaparib also accounts for the highest number of clinical trials; with single drug or in combination with other molecules.

Olaparib

Total Studies

153

Completed studies

23

Combinations (completed studies) : Olaparib+

Indication:

Rifampicin

Solid Tumours

Itraconazole

Pancreatic Cancer

Carboplatin

Cervical Cancer, Ovarian Cancer, Breast Cancer, Primary Peritoneal Cancer, Fallopian Tube Cancer, Endometrial Cancer

Gefitinib

Non Small Cell Lung Cancer

Irinotecan + Cisplatin + Carboplatin

Pancreatic Cancer

Bevacizumab

Neoplasm Metastasis

Paclitaxel

Advanced Solid Tumours

Carboplatin + Anthracycline + Cyclophosphamide

Breast Cancer

Dacarbazine

Melanoma Neoplasms

Irinotecan hydrochloride

Colorectal Cancer

Topotecan

Malignant Solid Tumors

Gemcitabine

Pancreatic Neoplasms

Cisplatin + Gemcitabine

Neoplasms

Niraparib

This is the second most researched PARP inhibitor. It is sold under brand name Zejula, marketed by Tesaro, Inc. (earlier developed by Merck). It is used as a maintenance treatment of recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in a complete or partial response to platinum-based chemotherapy. It is generally prescribed post chemotherapy in combination with cisplatin, oxaliplatin, carboplatin, or similar, if the patient responded to the mentioned drugs. It generated revenues of $218 million in 2016 as compared to $94 million in 2015.

Niraparib

Total Studies

26

Completed studies

3

Combinations (completed studies) : Nirparib+

Indication:

Temozolomide

Recurrence of Solid Tumor Glioblastoma MultiformeMelanoma

Rucaparib:

It is commercialized as Rubraca, and is marketed by Clovis Oncology (earlier, Pfizer Inc.). It is the third marketed PARP inhibitor used to treat advanced ovarian cancer. It is a monotherapy for treatment of patients with deleterious BRCA mutation (germline and/or somatic) associated advanced ovarian cancer who have been treated with 2 or more chemotherapies.

Rucaparib

Total Studies

16

Completed studies

3

Combinations (completed studies) : Rucaparib+

Indication:

Carboplatin

Advanced Solid Tumors

PARP Inhibitors 2017

Sources: Company websites, press releases, annual reports, SEC filings, drugs.com and clinicaltrial.gov.

PARP Inhibitors 2017 last edit: 2017-10-30T19:26:44+00:00 da Luca

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