talazoparib tosylate 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
poly-ADP-ribose polymerase inhibitors 5300 1207456-01-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • talazoparib tosylate
  • talazoparib
  • talzenna
  • BMN 673
  • BMN-673
  • BMN-673ts
  • LT 006673
  • LT-00673
  • LT-673
  • MDV-3800
Talazoparib is an inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, including PARP1 and PARP2, which play a role in DNA repair. In vitro studies with cancer cell lines that harbored defects in DNA repair genes, including BRCA 1 and 2, have shown that talazoparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complexes resulting in DNA damage, decreased cell proliferation, and apoptosis. Talazoparib anti-tumor activity was observed in human patient-derived xenograft breast cancer tumor models that expressed mutated or wild-type BRCA 1 and 2.
  • Molecular weight: 380.36
  • Formula: C19H14F2N6O
  • CLOGP: 0.62
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 2
  • TPSA: 84.20
  • ALOGS: -3.58
  • ROTB: 2
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
S (Water solubility) 0.02 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
June 20, 2019 EMA PFIZER EUROPE MA EEIG
Oct. 16, 2018 FDA PFIZER INC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Neoplasm progression 259.63 52.75 63 628 36365 63451966
Anaemia 165.55 52.75 74 617 293356 63194975
Thrombocytopenia 83.93 52.75 38 653 151119 63337212
Febrile neutropenia 63.14 52.75 29 662 118420 63369911
Pancytopenia 55.61 52.75 25 666 96908 63391423

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Anaemia 53.66 39.73 32 338 233303 34723258

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Neoplasm progression 227.40 45.35 63 946 51619 79691760
Anaemia 183.17 45.35 95 914 444920 79298459
Febrile neutropenia 96.02 45.35 50 959 230949 79512430
Thrombocytopenia 84.06 45.35 48 961 265211 79478168
Second primary malignancy 55.97 45.35 16 993 14334 79729045
Pancytopenia 47.00 45.35 28 981 165717 79577662
Haematotoxicity 46.03 45.35 14 995 15505 79727874

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01XK04 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Poly (ADP-ribose) polymerase (PARP) inhibitors
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D000067856 Poly(ADP-ribose) Polymerase Inhibitors
FDA MoA N0000191622 Poly(ADP-Ribose) Polymerase Inhibitors
FDA EPC N0000191623 Poly(ADP-Ribose) Polymerase Inhibitor

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Germline BRCA-mutated, HER2-negative metastatic breast cancer indication 767444009




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.23 acidic
pKa2 4.1 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 0.1MG BASE TALZENNA PFIZER N211651 June 20, 2023 RX CAPSULE ORAL 10780088 July 27, 2029 TREATMENT OF ADULT PATIENTS WITH HRR GENE-MUTATED METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC) IN COMBINATION WITH ENZALUTAMIDE
EQ 0.1MG BASE TALZENNA PFIZER N211651 June 20, 2023 RX CAPSULE ORAL 9820985 July 27, 2029 TREATMENT OF ADULT PATIENTS WITH DELETERIOUS OR SUSPECTED DELETERIOUS GERMLINE BREAST CANCER SUSCEPTIBILITY GENE (BRCA)-MUTATED (GBRCAM) HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE LOCALLY ADVANCED OR METASTATIC BREAST CANCER
EQ 0.25MG BASE TALZENNA PFIZER N211651 Oct. 16, 2018 RX CAPSULE ORAL 10780088 July 27, 2029 TREATMENT OF ADULT PATIENTS WITH HRR GENE-MUTATED METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC) IN COMBINATION WITH ENZALUTAMIDE
EQ 0.25MG BASE TALZENNA PFIZER N211651 Oct. 16, 2018 RX CAPSULE ORAL 9820985 July 27, 2029 TREATMENT OF ADULT PATIENTS WITH DELETERIOUS OR SUSPECTED DELETERIOUS GERMLINE BREAST CANCER SUSCEPTIBILITY GENE (BRCA)-MUTATED (GBRCAM) HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE LOCALLY ADVANCED OR METASTATIC BREAST CANCER
EQ 0.35MG BASE TALZENNA PFIZER N211651 June 20, 2023 RX CAPSULE ORAL 10780088 July 27, 2029 TREATMENT OF ADULT PATIENTS WITH HRR GENE-MUTATED METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC) IN COMBINATION WITH ENZALUTAMIDE
EQ 0.35MG BASE TALZENNA PFIZER N211651 June 20, 2023 RX CAPSULE ORAL 9820985 July 27, 2029 TREATMENT OF ADULT PATIENTS WITH DELETERIOUS OR SUSPECTED DELETERIOUS GERMLINE BREAST CANCER SUSCEPTIBILITY GENE (BRCA)-MUTATED (GBRCAM) HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE LOCALLY ADVANCED OR METASTATIC BREAST CANCER
EQ 0.5MG BASE TALZENNA PFIZER N211651 Sept. 20, 2021 RX CAPSULE ORAL 10780088 July 27, 2029 TREATMENT OF ADULT PATIENTS WITH HRR GENE-MUTATED METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC) IN COMBINATION WITH ENZALUTAMIDE
EQ 0.5MG BASE TALZENNA PFIZER N211651 Sept. 20, 2021 RX CAPSULE ORAL 9820985 July 27, 2029 TREATMENT OF ADULT PATIENTS WITH DELETERIOUS OR SUSPECTED DELETERIOUS GERMLINE BREAST CANCER SUSCEPTIBILITY GENE (BRCA)-MUTATED (GBRCAM) HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE LOCALLY ADVANCED OR METASTATIC BREAST CANCER
EQ 0.75MG BASE TALZENNA PFIZER N211651 Sept. 20, 2021 RX CAPSULE ORAL 9820985 July 27, 2029 TREATMENT OF ADULT PATIENTS WITH DELETERIOUS OR SUSPECTED DELETERIOUS GERMLINE BREAST CANCER SUSCEPTIBILITY GENE (BRCA)-MUTATED (GBRCAM) HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE LOCALLY ADVANCED OR METASTATIC BREAST CANCER
EQ 1MG BASE TALZENNA PFIZER N211651 Oct. 16, 2018 RX CAPSULE ORAL 9820985 July 27, 2029 TREATMENT OF ADULT PATIENTS WITH DELETERIOUS OR SUSPECTED DELETERIOUS GERMLINE BREAST CANCER SUSCEPTIBILITY GENE (BRCA)-MUTATED (GBRCAM) HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE LOCALLY ADVANCED OR METASTATIC BREAST CANCER

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 0.1MG BASE TALZENNA PFIZER N211651 June 20, 2023 RX CAPSULE ORAL Oct. 16, 2023 NEW CHEMICAL ENTITY
EQ 0.25MG BASE TALZENNA PFIZER N211651 Oct. 16, 2018 RX CAPSULE ORAL Oct. 16, 2023 NEW CHEMICAL ENTITY
EQ 0.35MG BASE TALZENNA PFIZER N211651 June 20, 2023 RX CAPSULE ORAL Oct. 16, 2023 NEW CHEMICAL ENTITY
EQ 0.5MG BASE TALZENNA PFIZER N211651 Sept. 20, 2021 RX CAPSULE ORAL Oct. 16, 2023 NEW CHEMICAL ENTITY
EQ 0.75MG BASE TALZENNA PFIZER N211651 Sept. 20, 2021 RX CAPSULE ORAL Oct. 16, 2023 NEW CHEMICAL ENTITY
EQ 1MG BASE TALZENNA PFIZER N211651 Oct. 16, 2018 RX CAPSULE ORAL Oct. 16, 2023 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Poly [ADP-ribose] polymerase 2 Enzyme INHIBITOR Ki 9.06 SCIENTIFIC LITERATURE DRUG LABEL
Poly [ADP-ribose] polymerase 1 Enzyme INHIBITOR Ki 8.92 SCIENTIFIC LITERATURE DRUG LABEL
Poly [ADP-ribose] polymerase 4 Enzyme Kd 9.15 CHEMBL
Tankyrase-1 Enzyme Kd 7.28 CHEMBL
Mono [ADP-ribose] polymerase PARP16 Unclassified Kd 6 CHEMBL
Poly [ADP-ribose] polymerase 10 Enzyme Kd 5.24 CHEMBL
Poly [ADP-ribose] polymerase 3 Enzyme Kd 7.62 CHEMBL

External reference:

IDSource
02WK9U5NZC UNII
C4726799 UMLSCUI
2YQ PDB_CHEM_ID
CHEMBL3137318 ChEMBL_ID
135565654 PUBCHEM_CID
CHEMBL3137320 ChEMBL_ID
D10732 KEGG_DRUG
C586365 MESH_SUPPLEMENTAL_RECORD_UI
8313 IUPHAR_LIGAND_ID
DB11760 DRUGBANK_ID
017808 NDDF
017809 NDDF
1193867007 SNOMEDCT_US
782199007 SNOMEDCT_US
782211002 SNOMEDCT_US
4037929 VANDF
9868 INN_ID
1373431-65-2 SECONDARY_CAS_RN
2099703 RXNORM
294344 MMSL
35314 MMSL
d09010 MMSL

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Talzenna HUMAN PRESCRIPTION DRUG LABEL 1 0069-0296 CAPSULE 0.25 mg ORAL NDA 31 sections
Talzenna HUMAN PRESCRIPTION DRUG LABEL 1 0069-0296 CAPSULE 0.25 mg ORAL NDA 31 sections
Talzenna HUMAN PRESCRIPTION DRUG LABEL 1 0069-1031 CAPSULE 0.10 mg ORAL NDA 31 sections
Talzenna HUMAN PRESCRIPTION DRUG LABEL 1 0069-1195 CAPSULE 1 mg ORAL NDA 31 sections
Talzenna HUMAN PRESCRIPTION DRUG LABEL 1 0069-1195 CAPSULE 1 mg ORAL NDA 31 sections
Talzenna HUMAN PRESCRIPTION DRUG LABEL 1 0069-1235 CAPSULE 0.35 mg ORAL NDA 31 sections
Talzenna HUMAN PRESCRIPTION DRUG LABEL 1 0069-1501 CAPSULE 0.50 mg ORAL NDA 31 sections
Talzenna HUMAN PRESCRIPTION DRUG LABEL 1 0069-1501 CAPSULE 0.50 mg ORAL NDA 31 sections
Talzenna HUMAN PRESCRIPTION DRUG LABEL 1 0069-1751 CAPSULE 0.75 mg ORAL NDA 31 sections
Talzenna HUMAN PRESCRIPTION DRUG LABEL 1 0069-1751 CAPSULE 0.75 mg ORAL NDA 31 sections
Talzenna HUMAN PRESCRIPTION DRUG LABEL 1 63539-051 CAPSULE 0.50 mg ORAL NDA 31 sections
Talzenna HUMAN PRESCRIPTION DRUG LABEL 1 63539-295 CAPSULE 1 mg ORAL NDA 31 sections
Talzenna HUMAN PRESCRIPTION DRUG LABEL 1 63539-295 CAPSULE 1 mg ORAL NDA 31 sections