Drug Details

General Information of the Drug (ID: DR6756)
Name
Olaparib
Synonyms
Olaparib; 763113-22-0; AZD2281; Lynparza; KU-0059436; AZD 2281; AZD-2281; 1-(Cyclopropylcarbonyl)-4-[5-[(3,4-dihydro-4-oxo-1-phthalazinyl)methyl]-2-fluorobenzoyl]piperazine; Olaparib (AZD2281, Ku-0059436); 4-(3-(4-(Cyclopropanecarbonyl)piperazine-1-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one; UNII-WOH1JD9AR8; KU-59436; AZD2281(olaparib); MFCD13185161; WOH1JD9AR8; Olaparib (AZD-2281); 4-[[3-[4-(Cyclopropanecarbonyl)piperazine-1-carbonyl]-4-fluorophenyl]methyl]-2H-phthalazin-1-one; C24H23FN4O3; CHEBI:83766; AZ2281; 4-(3-{[4-(Cyclopropylcarbonyl)piperazin-1-Yl]carbonyl}-4-Fluorobenzyl)phthalazin-1(2h)-One; 4-[3-(4-Cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one; 937799-91-2; KU59436; 4-[3-[4-(Cyclopropanecarbonyl)piperazine-1-carbonyl]-4-fluorobenzyl]phthalazin-1(2H)-one; 4-[(3-{[4-(Cyclopropylcarbonyl)piperazin-1-yl]carbonyl}-4-fluorophenyl)methyl]phthalazin-1(2H)-one; OLAPARIB cpd; Olaparib [USAN:INN]; Acylpiperazine analogue, 47; Olaparibum; AZD221; Lynparza (TN); 09L; 4-((3-{(4-(cyclopropylcarbonyl)piperazin-1-yl)carbonyl}-4-fluorophenyl)methyl)phthalazin-1(2H)-one; PubChem19148; KU 59436; Olaparib (AZD2281); Olaparib - AZD2281; cc-16; AZD-2281 (Olaparib); Olaparib (JAN/USAN/INN); MLS006010185; SCHEMBL426568; CHEMBL521686; GTPL7519; BDBM27566; AOB1085; DTXSID60917988; EX-A002; BCPP000360; HMS3295I09; HMS3426C03; HMS3654G13; HMS3746K07; HMS3870H03; AMY10295; BCP01872; ABP000423; ANW-43329; NSC747856; NSC753686; s1060; ZINC40430143; AKOS005145764; AC-7939; ACN-032229; AZ-2281; BCP9000363; CCG-264799; CS-0075; DB09074; EX-7210; KEYLYNK-010 COMPONENT OLAPARIB; NSC 747856; NSC-747856; NSC-753686; QC-2660; SB14617; SS-4573; AZD2281,Olaparib, KU-0059436; NCGC00238451-01; NCGC00238451-02; NCGC00238451-09; NCGC00238451-11; 4-[(3-{[4-Cyclopropylcarbonyl)piperazin-4-yl]carbonyl}-4-fluorophenyl)methyl]phtalazin-1(2H)-one; AK-40514; HY-10162; Olaparib (AZD2281, KU0059436); SMR004701291; SY040527; OLAPARIB COMPONENT OF KEYLYNK-010; AB0009952; Olaparib(AZD2281,KuDOSKU-0059436); A9666; BB 0260909; FT-0651458; KU 0059436; SW218142-2; EC-000.2324; D09730; S-3781; S-7836; Z-3275; AZD2281(olaparib)/AZD-2281/KU0059436; J-503540; Q7083106; BRD-K02113016-001-08-9; BRD-K02113016-001-09-7; AZD 2281; ; ; KU 0059436; ; ; KU 59436; 1-(cyclopropylcarbonyl)-4-[5-[(3,4-dihydro-4-oxo-1-phthalazine; 4-(3-(1-(cyclopropanecarbonyl)piperazine-4-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one; (2H)-Phthalazinone, 4-((3-((4-(cyclopropylcarbonyl)-1-piperazinyl)carbonyl)-4-fluorophenyl)methyl)-; [4-(Cyclopropanecarbonyl)piperazin-1-yl]{2-fluoro-5-[(4-hydroxyphthalazin-1-yl)methyl]phenyl}methanone; 1(2H)-Phthalazinone, 4-[[3-[[4-(cyclopropylcarbonyl)-1-piperazinyl]carbonyl]-4-fluorophenyl]methyl]-; 1021843-02-6; 4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbonyl]-4-fluorophenyl}methyl)-1,2-dihydrophthalazin-1-one; 4-{[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorophenyl]methyl}-1,2-dihydrophthalazin-1-one
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Molecular Type
Small molecule
Disease Ovarian cancer [ICD-11: 2C73] Approved [1]
Structure
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2D MOL

3D MOL

ADMET Property
Absorption AUC
The area under the plot of plasma concentration (AUC) of drug is 25.8 mcgh/L
Absorption Cmax
The maximum plasma concentration (Cmax) of drug is 4.7 and 9.1 mg/L
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 1-3 h
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability
Clearance
The total clearance of drug is 4.6 L/h
Elimination
Approximately 86% of the administered dose is recovered after 7 days from which 44% is found in the urine and 42% is obtained in feces
Half-life
The concentration or amount of drug in body reduced by one-half in 5 - 11 hours
Metabolism
The drug is metabolized via the liver
Vd
The volume of distribution (Vd) of drug is 40.3 L
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    Click to Show/Hide the Molecular Information and External Link(s) of This Natural Product
Formula
C24H23FN4O3
PubChem CID
23725625
Canonical SMILES
C1CC1C(=O)N2CCN(CC2)C(=O)C3=C(C=CC(=C3)CC4=NNC(=O)C5=CC=CC=C54)F
InChI
1S/C24H23FN4O3/c25-20-8-5-15(14-21-17-3-1-2-4-18(17)22(30)27-26-21)13-19(20)24(32)29-11-9-28(10-12-29)23(31)16-6-7-16/h1-5,8,13,16H,6-7,9-12,14H2,(H,27,30)
InChIKey
FDLYAMZZIXQODN-UHFFFAOYSA-N
CAS Number
CAS 763113-22-0
ChEBI ID
CHEBI:83766
TTD Drug ID
D0J9HW
DrugBank ID
DB09074
Combinatorial Therapeutic Effect(s) Validated Clinically or Experimentally
    α. A List of Natural Product(s) Able to Enhance the Efficacy of This Drug
          Metformin      Galega officinalis     Click to Show/Hide the Molecular Data of This NP
                 Achieving Therapeutic Synergy     Click to Show/Hide
                    Representative Experiment Reporting the Effect of This Combination [2]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Molecule(s)
                    Regulation		 Down-regulation Expression PARP1  Molecule Info 
Pathway MAP
                    In-vitro Model UWB1.289 CVCL_B079 BRCA1 syndrome Homo sapiens
UWB1.289+BRCA1 CVCL_B078 BRCA1 syndrome Homo sapiens
SK-OV-3 CVCL_0532 Ovarian serous cystadenocarcinoma Homo sapiens
OVCAR-3 CVCL_0465 Ovarian serous adenocarcinoma Homo sapiens
A2780 CVCL_0134 Ovarian endometrioid adenocarcinoma Homo sapiens
                    Experimental
                    Result(s)		 Combining PARP inhibitors with metformin enhances its anti-proliferative activity in BRCA mutant ovarian cancer cells.
    β. A List of Natural Product(s) Able to Decrease the Adverse Effect of This Drug
          Daunorubicin      Streptomyces peucetius     Click to Show/Hide the Molecular Data of This NP
                 Decreasing Adverse Drug Reaction     Click to Show/Hide
                    Representative Experiment Reporting the Effect of This Combination [3]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    In-vitro Model KG-1a CVCL_1824 Adult acute myeloid leukemia Homo sapiens
Hep-G2 CVCL_0027 Hepatocellular carcinoma Homo sapiens
                    Experimental
                    Result(s)		 Olaparib interferes with anthracycline metabolism, and suggest that this phenomenon might be utilized for combating anthracycline resistance.
Target and Pathway
Target(s) Poly [ADP-ribose] polymerase (PARP)  Molecule Info  [4]
References
Reference 1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7519).
Reference 2 Preclinical evaluation of olaparib and metformin combination in BRCA1 wildtype ovarian cancer. Gynecol Oncol. 2016 Aug;142(2):323-31.
Reference 3 Olaparib Synergizes the Anticancer Activity of Daunorubicin via Interaction with AKR1C3. Cancers (Basel). 2020 Oct 26;12(11):3127.
Reference 4 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
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