Olaparib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2014
- First approval year
- 2014
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Olaparib
- Molecular weight
- 434.47
- Structure (SMILES)
- O=C(c1cc(Cc2n[nH]c(=O)c3ccccc23)ccc1F)N1CCN(C(=O)C2CC2)CC1
- lynparza
- Lynparza
- az 2281
- AZ-2281
- az2281
- AZ2281
- az2281 carboplatin
- azd 2281
- AZD 2281
- AZD-2281
- azd2281
- AZD2281
- DWC202510 (Olaparib 150mg)
- DWZ2501 (Olaparib 150mg)
- keylynk 010 component olaparib
- KEYLYNK-010 COMPONENT OLAPARIB
- ku 0059436
- ku 59436
- KU-0059436
- KU-0059436 (AZD2281)(PARP inhibitor)
- KU-59436
- ku0059436
- KU0059436
- lynparza
- Lynparza
- LYNPARZA
- Lynparza® (AstraZeneca Pharma Poland Sp. z o.o.)
And 38 more, listed on the interactive page.
- ATC classification codes
- L01XK01
Sources for recorded values
- CAS registry numbers
- 763113-22-0
- ChEMBL ID
- CHEMBL521686
- InChIKey
- FDLYAMZZIXQODN-UHFFFAOYSA-N
- PubChem compound IDs
- 23725625
- RxNorm IDs (RxCUI)
- 1597582
- FDA ingredient codes (UNII)
- WOH1JD9AR8
- Applicant
- ASTRAZENECA
- Approval date
- 17 Aug 2017
- Application number
- NDA208558
- Status
- Authorised
- Status date
- 16 Dec 2014
- Authorisation date
- 16 Dec 2014
- Approved indications
- Ovarian cancer Lynparza is indicated as monotherapy for the: maintenance treatment of adult patients with advanced (FIGO stages III and IV) BRCA1/2-mutated (germline and/or somatic) high-grade epithelial ovarian, fallopian tube or primary peritoneal cancer who are in response (complete or partial) following completion of first-line platinum-based chemotherapy. maintenance treatment of adult patients with platinum sensitive relapsed high grade epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in response (complete or partial) to platinum based chemotherapy. Lynparza in combination with bevacizumab is indicated for the: maintenance treatment of adult patients with advanced (FIGO stages III and IV) high-grade epithelial ovarian, fallopian tube or primary peritoneal cancer who are in response (complete or partial) following completion of first-line platinum-based chemotherapy in combination with bevacizumab and whose cancer is associated with homologous recombination deficiency (HRD) positive status defined by either a BRCA1/2 mutation and/or genomic instability (see section 5.1). Breast cancer Lynparza is indicated as: monotherapy or in combination with endocrine therapy for the adjuvant treatment of adult patients with germline BRCA1/2-mutations who have HER2-negative, high risk early breast cancer previously treated with neoadjuvant or adjuvant chemotherapy (see sections 4.2 and 5.1). monotherapy for the treatment of adult patients with germline BRCA1/2-mutations, who have HER2 negative locally advanced or metastatic breast cancer. Patients should have previously been treated with an anthracycline and a taxane in the (neo)adjuvant or metastatic setting unless patients were not suitable for these treatments (see section 5.1). Patients with hormone receptor (HR)-positive breast cancer should also have progressed on or after prior endocrine therapy, or be considered unsuitable for endocrine therapy. Adenocarcinoma of the pancreas Lynparza is indicated as: monotherapy for the maintenance treatment of adult patients with germline BRCA1/2-mutations who have metastatic adenocarcinoma of the pancreas and have not progressed after a minimum of 16 weeks of platinum treatment within a first-line chemotherapy regimen. Prostate cancer Lynparza is indicated as: monotherapy for the treatment of adult patients with metastatic castration-resistant prostate cancer (mCRPC) and BRCA1/2-mutations (germline and/or somatic) who have progressed following prior therapy that included a new hormonal agent. in combination with abiraterone and prednisone or prednisolone for the treatment of adult patients with mCRPC in whom chemotherapy is not clinically indicated (see section 5.1). Endometrial cancer Lynparza in combination with durvalumab is indicated for the maintenance treatment of adult patients with primary advanced or recurrent endometrial cancer that is mismatch repair proficient (pMMR) whose disease has not progressed on first-line treatment with durvalumab in combination with carboplatin and paclitaxel.
- Product number
- EMEA/H/C/003726
- Authorisation holder
- AstraZeneca AB
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- No
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Breast Neoplasms
- Ovarian Neoplasms
- Pancreatic Neoplasms
- Prostatic Neoplasms, Castration-Resistant
European medicines record
- Patents
- 14
- Designations
- 5
- Earliest recorded loss of exclusivity
- 25 Oct 2041
- First in class
- Yes
- Fast track
- No
- Breakthrough designation
- Yes
- Orphan designation
- No
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- Yes
- Availability
- Prescription only
- Pharmacology name
- olaparib
- Type
- Synthetic organic
- Drug name stem
- -parib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- poly(ADP-ribose) polymerase 1
- Gene symbol
- PARP1
- Protein identifier
- P09874
- Median affinity
- 8.3
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- poly(ADP-ribose) polymerase 2
- Gene symbol
- PARP2
- Protein identifier
- Q9UGN5
- Median affinity
- 9
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- poly (ADP-ribose) polymerase 3
- Gene symbol
- PARP3
- Protein identifier
- Q9Y6F1
- Median affinity
- 8.24
- Affinity units
- pKd
- Mechanism
- PARP 1, 2 and 3 inhibitor
- Action type
- Inhibitor
- Target
- PARP 1, 2 and 3
- Protein identifier
- P09874
- Mechanism
- PARP 1, 2 and 3 inhibitor
- Action type
- Inhibitor
- Target
- PARP 1, 2 and 3
- Protein identifier
- Q9UGN5
- Mechanism
- PARP 1, 2 and 3 inhibitor
- Action type
- Inhibitor
- Target
- PARP 1, 2 and 3
- Protein identifier
- Q9Y6F1
Open Targets mechanisms
- Mechanism
- PARP 1, 2 and 3 inhibitor
- Action type
- Inhibitor
- Target
- PARP 1, 2 and 3
- Action type
- Inhibitor
- Gene symbol
- PARP1
- Protein identifier
- P09874
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- PARP2
- Protein identifier
- Q9UGN5
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- PARP3
- Protein identifier
- Q9Y6F1
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Leukemia, Lymphocytic, Chronic, B-Cell
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000095
- Subject identifier
- D015451
- Condition
- Sarcoma, Ewing
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000174
- Subject identifier
- D012512
- Condition
- Carcinoma, Squamous Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000181
- Subject identifier
- D002294
- Condition
- Prostatic Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000196
- Subject identifier
- D011471
- Condition
- Myelodysplastic Syndromes
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000198
- Subject identifier
- D009190
- Condition
- Squamous Cell Carcinoma of Head and Neck
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000199
- Subject identifier
- D000077195
- Condition
- Lymphoma, T-Cell, Peripheral
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000211
- Subject identifier
- D016411
- Condition
- Leukemia, Myeloid, Acute
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000222
- Subject identifier
- D015470
- Condition
- Pheochromocytoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000239
- Subject identifier
- D010673
- Condition
- Urinary Bladder Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000294
- Subject identifier
- D001749
- Condition
- Breast Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000305
- Subject identifier
- D001943
- Condition
- Carcinoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000313
- Subject identifier
- D002277
- Condition
- Stomach Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000503
- Subject identifier
- D013274
- Condition
- Neoplasms, Germ Cell and Embryonal
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000514
- Subject identifier
- D009373
- Condition
- Glioblastoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000519
- Subject identifier
- D005909
- Condition
- Leiomyosarcoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000564
- Subject identifier
- D007890
- Condition
- Lymphoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000574
- Subject identifier
- D008223
- Condition
- Mesothelioma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000588
- Subject identifier
- D008654
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Osteosarcoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000637
- Subject identifier
- D012516
- Condition
- Prostatic Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000673
- Subject identifier
- D011471
- Condition
- Carcinoma, Renal Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000681
- Subject identifier
- D002292
- Condition
- Sarcoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000691
- Subject identifier
- D012509
- Condition
- Small Cell Lung Carcinoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000702
- Subject identifier
- D055752
- Condition
- Carcinoma, Squamous Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000707
- Subject identifier
- D002294
And 53 more, listed on the interactive page.
- Condition identifier
- EFO_0000174
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000181
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000198
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000211
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000222
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000305
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000503
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000514
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000519
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000574
- Highest recorded phase
- 1
- Condition identifier
- EFO_0000588
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0000637
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000673
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000681
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000691
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000702
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000756
- Highest recorded phase
- 2
- Condition identifier
- EFO_0001075
- Condition identifier
- EFO_0001361
- Condition identifier
- EFO_0001663
- Highest recorded phase
- 2
- Condition identifier
- EFO_0002617
- Highest recorded phase
- 2
- Condition identifier
- EFO_0002618
- Highest recorded phase
- 3
- Condition identifier
- EFO_0002916
- Highest recorded phase
- 1
- Condition identifier
- EFO_0003060
- Highest recorded phase
- 3
And 109 more, listed on the interactive page.
- Event
- acute myeloid leukaemia
- Reports
- 113
- Reporting signal score
- 342.629
- Event
- anaemia
- Reports
- 390
- Reporting signal score
- 544.88
- Event
- blood creatinine increased
- Reports
- 55
- Reporting signal score
- 35.1282
- Event
- bone marrow failure
- Reports
- 45
- Reporting signal score
- 53.6277
- Event
- carbohydrate antigen 125 increased
- Reports
- 52
- Reporting signal score
- 206.64
- Event
- disease progression
- Reports
- 108
- Reporting signal score
- 103.383
- Event
- fall
- Reports
- 8
- Reporting signal score
- 30.0842
- Event
- haematotoxicity
- Reports
- 31
- Reporting signal score
- 53.1936
- Event
- ileus
- Reports
- 33
- Reporting signal score
- 50.5849
- Event
- interstitial lung disease
- Reports
- 88
- Reporting signal score
- 111.63
- Event
- malignant neoplasm progression
- Reports
- 421
- Reporting signal score
- 1,102.93
- Event
- metastases to central nervous system
- Reports
- 26
- Reporting signal score
- 42.4846
- Event
- metastases to liver
- Reports
- 36
- Reporting signal score
- 61.9878
- Event
- metastases to lymph nodes
- Reports
- 19
- Reporting signal score
- 35.7365
- Event
- metastases to peritoneum
- Reports
- 21
- Reporting signal score
- 62.5552
- Event
- metastases to pleura
- Reports
- 10
- Reporting signal score
- 31.1856
- Event
- myelodysplastic syndrome
- Reports
- 149
- Reporting signal score
- 447.905
- Event
- myelosuppression
- Reports
- 38
- Reporting signal score
- 66.9023
- Event
- nausea
- Reports
- 255
- Reporting signal score
- 59.8828
- Event
- neutrophil count decreased
- Reports
- 57
- Reporting signal score
- 58.8383
- Event
- ovarian cancer recurrent
- Reports
- 38
- Reporting signal score
- 167.579
- Event
- pancytopenia
- Reports
- 76
- Reporting signal score
- 76.3664
- Event
- pneumonitis
- Reports
- 52
- Reporting signal score
- 71.6327
- Event
- renal impairment
- Reports
- 56
- Reporting signal score
- 30.4091
- Event
- thrombocytopenia
- Reports
- 88
- Reporting signal score
- 41.1697
And 1 more, listed on the interactive page.
- NCT00494234
- NCT01042379
- NCT03109080
- NCT03594396
- NCT03740893
- NCT04191135
- NCT00494442
- NCT00516373
- NCT00628251
- NCT03314740
- NCT00515866
- NCT00516438
- NCT00516802
- NCT00777582
- NCT00782574
- NCT00819221
- NCT01851265
- NCT01894243
- NCT01894256
- NCT01900028
- NCT01921140
- NCT01929603
- NCT02029001
- NCT02093351
- NCT02430311
And 250 more, listed on the interactive page.
- Hydrogen bond acceptors
- 4
- Hydrogen bond donors
- 1
- Polar surface area
- 86.37
- Calculated partition coefficient (ALogP)
- 2.35
- Calculated partition coefficient (XLogP)
- 1.9
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 4
- Heavy atoms
- 32
- Molecular formula
- C24H23FN4O3
- Monoisotopic mass
- 434.17541877
- Natural product
- No
- 0310-0569
- 0310-0578
- 0310-0668
- 0310-0679
- Recorded assays
- 6,589
- Active assays
- 575
- Confirmatory
- Other
- Screening
- Poly(ADP-ribose) Polymerase Inhibitors
- Antineoplastic Agents
These details could not be displayed.
Related records
Trials (423)
- 177Lu-DOTA-TATE and Olaparib in Somatostatin Receptor Positive Tumours
- 177Lu-PSMA-617 Therapy and Olaparib in Patients With Metastatic Castration Resistant Prostate Cancer
- A Bioequivalence Study to Evaluate Pharmacokinetics and Safety of BR2022 and BR2022-1 in Patients With Deleterious or Suspected Deleterious Germline BRCA-Mutated Advanced Ovarian Cancer
- A Clinical Study of Boserolimab (MK-5890) With Pembrolizumab and Chemotherapy in People With Early Triple-Negative Breast Cancer (MK-5890-003)
- A Clinical Study of Sacituzumab Tirumotecan (Sac-TMT, MK-2870) in People With Breast Cancer (MK-2870-032)
- A Crossover Bioequivalence Study of Olaparib Tablets, 150 mg (Lek Pharmaceuticals d.d.) and Lynparza® (Olaparib) Tablets 150 mg (AstraZeneca Pharmaceuticals LP), in Patients With Breast Cancer Gene (BRCA) Mutated Ovarian Cancer, Recurrent Ovarian Cancer or Metastatic Breast Cancer
- A Dye for the Detection of Cancer of the Tongue and Mouth
- A Phase 1 Study of RO7623066 Alone and in Combination in Patients With Advanced Solid Tumors
- A Phase 1 Study of XL309 (ISM3091) Alone and in Combination in Participants With Advanced Solid Tumors
- A Phase 2 Study of Cediranib in Combination With Olaparib in Advanced Solid Tumors
- A Phase I, Open-Label, 2 Part Multicentre Study to Assess the Safety and Efficacy of Olaparib in Combination With Carboplatin in Patients With Advanced HER-2 Negative Breast Cancer
- A Phase I/II Study of MEDI4736 in Combination With Olaparib in Patients With Advanced Solid Tumors.
- A Phase II Clinical Trial Evaluating the Combination of Olaparib and Temozolomide for the Treatment of Advanced Uterine Leiomyosarcoma
- A Phase II Clinical Trial of Cediranib and Olaparib Maintenance in Advanced Recurrent Cervical Cancer
- A Phase II Randomized Study Comparing the Efficacy and Safety of Targeted Therapy or Cancer Immunotherapy Versus Platinum-Based Chemotherapy in Patients With Cancer of Unknown Primary Site
- A Phase II, Study to Determine the Preliminary Efficacy of Novel Combinations of Treatment in Patients With Platinum Refractory Extensive-Stage Small-Cell Lung Cancer
- A Phase III Randomised Study to Evaluate Dato-DXd and Durvalumab for Neoadjuvant/Adjuvant Treatment of Triple-Negative or Hormone Receptor-low/HER2-negative Breast Cancer
- A Platform Study of Novel Agents in Combination With Radiotherapy in NSCLC
- A Study Evaluating the Efficacy and Safety of Biomarker-Driven Therapies in Patients With Persistent or Recurrent Rare Epithelial Ovarian Tumors
- A Study of BL-B01D1 Combination Therapy in Patients With Metastatic Castration-resistant Prostate Cancer
Approved for (12)
- Breast cancer
- Breast carcinoma
- Breast neoplasm
- Cancer
- Exocrine pancreatic carcinoma
- Neoplasm
- Ovarian cancer
- Ovarian carcinoma
- Ovarian neoplasm
- Pancreatic neoplasm
- Prostate cancer
- Prostate carcinoma
In development for (66)
- Acute myeloid leukemia Phase 2
- Adrenal gland pheochromocytoma Phase 2
- Angiosarcoma Phase 2
- B-cell chronic lymphocytic leukemia Phase 1
- Bile duct cancer Phase 2
- Biliary tract cancer Phase 2
- Carcinoma Phase 3
- Carcinoma of esophagus Phase 1
- Carcinosarcoma Phase 2
- Central nervous system neoplasm Phase 1
- Cervical cancer Phase 2
- Cervical carcinoma Phase 2
- Cholangiocarcinoma Phase 2
- Colorectal cancer Phase 2
- Endometrial cancer Phase 3
- Endometrial carcinoma Phase 3
- Ewing sarcoma Phase 2
- Fallopian tube cancer Phase 2
- Fallopian tube carcinoma Phase 2
- Gastric adenocarcinoma Phase 3