Olaparib

Olaparib Brand Name– Lynparza

What is Olaparib

Olaparib is an oral poly (ADP-ribose) polymerase (PARP) inhibitor. PARP enzymes are involved in normal cellular homeostasis, including DNA transcription, cell cycle regulation, and DNA repair. Increased cytotoxicity and anti-tumor activity has been noted in cell lines and mouse tumor models with deficiencies in BRCA.

It is approved by the FDA for the treatment of germline or somatic BRCA-mutated (gBRCAm or sBRCAm) or suspected gBRCAm or sBRCAm advanced ovarian cancer in patients who have failed 3 or more prior courses of chemotherapy and for HER2-negative, gBRCAm metastatic breast cancer in patients previously treated with chemotherapy in the neoadjuvant, adjuvant, or metastatic setting, and metastatic castration-resistant prostate cancer in patients with a homologous recombination repair (HRR) gene mutation.

It is approved for maintenance therapy as a single agent after a response to platinum-based chemotherapy in patients with advanced BRCA-mutated ovarian cancer and in patients with gBRCAm or suspected gBRCAm metastatic pancreatic cancer.

It is also approved as first-line maintenance therapy for platinum-sensitive advanced ovarian cancer that is associated with a homologous recombination deficiency (HRD) in combination with bevacizumab.

The most common adverse reactions include anemia, nausea, fatigue, vomiting, upper respiratory infection, diarrhea, and arthralgia/myalgia.

Indications

  1. breast cancer
  2. ovarian cancer
  3. pancreatic cancer
  4. prostate cancer

For the treatment of ovarian cancer

for the first-line maintenance treatment of deleterious or suspected deleterious germline or somatic BRCA mutated (gBRCAm or sBRCAm) advanced epithelial ovarian, fallopian tube, or primary peritoneal cancer in patients who are in a complete or partial response to first-line platinum-based chemotherapy, as monotherapy

Side Effects

  1. abdominal pain
  2. abdominal pain
  3. anemia
  4. anemia
  5. anorexia
  6. anorexia
  7. arthralgia
  8. arthralgia
  9. asthenia
  10. back pain
  11. colitis
  12. constipation
  13. constipation
  14. cough
  15. cystitis
  16. diarrhea
  17. diarrhea
  18. dizziness
  19. dysgeusia
  20. dyspepsia
  21. dyspnea
  22. dyspnea
  23. edema
  24. erythema
  25. fatigue
  26. fatigue
  27. fever
  28. GI perforation
  29. headache
  30. headache
  31. hypomagnesemia
  32. infection
  33. infection
  34. influenza
  35. lethargy
  36. leukopenia
  37. leukopenia
  38. lymphopenia
  39. malaise
  40. musculoskeletal pain
  41. myalgia
  42. nausea
  43. nausea
  44. neutropenia
  45. neutropenia
  46. new primary malignancy
  47. oral ulceration
  48. peripheral edema
  49. peripheral neuropathy
  50. pharyngitis
  51. pneumonitis
  52. pulmonary embolism
  53. rash
  54. renal failure (unspecified)
  55. rhinitis
  56. sinusitis
  57. stomatitis
  58. stomatitis
  59. stroke
  60. thrombocytopenia
  61. thrombocytopenia
  62. thromboembolism
  63. vomiting
  64. vomiting

Monitoring Parameters

  • CBC with differential
  • pregnancy testing

Contraindications

  • bone marrow suppression
  • breast-feeding
  • chemotherapy
  • chronic lung disease (CLD)
  • contraception requirements
  • male-mediated teratogenicity
  • new primary malignancy
  • pneumonitis
  • pregnancy
  • pregnancy testing
  • pulmonary disease
  • radiation therapy
  • reproductive risk
  • thromboembolic disease
  • thromboembolism

Interactions

  • Acetaminophen; Butalbital
  • Acetaminophen; Butalbital; Caffeine
  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Amiodarone
  • Amobarbital
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Apalutamide
  • Aprepitant, Fosaprepitant
  • Aspirin, ASA; Butalbital; Caffeine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Atazanavir
  • Atazanavir; Cobicistat
  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Bexarotene
  • Bosentan
  • Butabarbital
  • Carbamazepine
  • Cenobamate
  • Ceritinib
  • Chloramphenicol
  • Ciprofloxacin
  • Clarithromycin
  • Cobicistat
  • Conivaptan
  • Crizotinib
  • Cyclosporine
  • Dabrafenib
  • Danazol
  • Darunavir
  • Darunavir; Cobicistat
  • Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Delavirdine
  • Dexamethasone
  • Diltiazem
  • Dronedarone
  • Duvelisib
  • Efavirenz
  • Efavirenz; Emtricitabine; Tenofovir
  • Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
  • Elagolix
  • Elagolix; Estradiol; Norethindrone acetate
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
  • Enzalutamide
  • Erythromycin
  • Erythromycin; Sulfisoxazole
  • Eslicarbazepine
  • Etravirine
  • Fedratinib
  • Fluconazole
  • Fluvoxamine
  • Fosamprenavir
  • Fosphenytoin
  • grapefruit juice
  • Idelalisib
  • Imatinib
  • Indinavir
  • Isavuconazonium
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Itraconazole
  • Ketoconazole
  • Lefamulin
  • Letermovir
  • Lopinavir; Ritonavir
  • Lorlatinib
  • Lumacaftor; Ivacaftor
  • Mephobarbital
  • Methohexital
  • Mifepristone
  • Mitotane
  • Modafinil
  • Nafcillin
  • Nefazodone
  • Nelfinavir
  • Netupitant, Fosnetupitant; Palonosetron
  • Nevirapine
  • Nilotinib
  • Ombitasvir; Paritaprevir; Ritonavir
  • Omeprazole; Amoxicillin; Rifabutin
  • Pentobarbital
  • Phenobarbital
  • Phenytoin
  • Posaconazole
  • Primidone
  • Ribociclib
  • Ribociclib; Letrozole
  • Rifabutin
  • Rifampin
  • Rifapentine
  • Rifaximin
  • Ritonavir
  • Saquinavir
  • Secobarbital
  • St. John’s Wort, Hypericum perforatum
  • Telithromycin
  • Thiopental
  • Tipranavir
  • Trandolapril; Verapamil
  • Tucatinib
  • Verapamil
  • Voriconazole
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