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

Stem definitionDrug idCAS RN
phosphatidylinositol 3-kinase inhibitors, antineoplastics 5296 1201438-56-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • duvelisib
  • copiktra
  • IPI-145
  • INK-1197
  • ABBV-954
Duvelisib is an inhibitor of PI3K with inhibitory activity predominantly against PI3K-delta and PI3K-gamma isoforms expressed in normal and malignant B-cells. Duvelisib induced growth inhibition and reduced viability in cell lines derived from malignant B-cells and in primary CLL tumor cells. Duvelisib inhibits several key cell-signaling pathways, including B-cell receptor signaling and CXCR12-mediated chemotaxis of malignant B-cells. Additionally, duvelisib inhibits CXCL12-induced T cell migration and M-CSF and IL-4 driven M2 polarization of macrophages.
  • Molecular weight: 416.87
  • Formula: C22H17ClN6O
  • CLOGP: 4.09
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 2
  • TPSA: 86.80
  • ALOGS: -4.33
  • ROTB: 4
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
50 mg O

ADMET properties:

PropertyValueReference
S (Water solubility) 0.02 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
May 19, 2021 EMA Verastem Europe GmbH
Sept. 24, 2018 FDA VERASTEM INC

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EM04 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Phosphatidylinositol-3-kinase (Pi3K) inhibitors

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

DiseaseRelationSNOMED_IDDOID
Chronic lymphoid leukemia, disease indication 92814006
Malignant lymphoma - small lymphocytic indication 302841002
Follicular non-Hodgkin's lymphoma indication 308121000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.52 acidic
pKa2 4.74 Basic
pKa3 4.04 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
15MG COPIKTRA SECURA N211155 Sept. 24, 2018 RX CAPSULE ORAL 9216982 Jan. 5, 2029 FOR THE TREATMENT OF PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) AND/OR SMALL LYMPHOCYTIC LEUKEMIA (SLL)
15MG COPIKTRA SECURA N211155 Sept. 24, 2018 RX CAPSULE ORAL 9216982 Jan. 5, 2029 FOR THE TREATMENT OF PATIENTS WITH FOLLICULAR LYMPHOMA (FL)
25MG COPIKTRA SECURA N211155 Sept. 24, 2018 RX CAPSULE ORAL 9216982 Jan. 5, 2029 FOR THE TREATMENT OF PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) AND/OR SMALL LYMPHOCYTIC LEUKEMIA (SLL)
25MG COPIKTRA SECURA N211155 Sept. 24, 2018 RX CAPSULE ORAL 9216982 Jan. 5, 2029 FOR THE TREATMENT OF PATIENTS WITH FOLLICULAR LYMPHOMA (FL)
15MG COPIKTRA SECURA N211155 Sept. 24, 2018 RX CAPSULE ORAL 9840505 Jan. 10, 2032 FOR THE TREATMENT OF PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) AND/OR SMALL LYMPHOCYTIC LEUKEMIA (SLL)
15MG COPIKTRA SECURA N211155 Sept. 24, 2018 RX CAPSULE ORAL 9840505 Jan. 10, 2032 FOR THE TREATMENT OF PATIENTS WITH FOLLICULAR LYMPHOMA (FL)
25MG COPIKTRA SECURA N211155 Sept. 24, 2018 RX CAPSULE ORAL 9840505 Jan. 10, 2032 FOR THE TREATMENT OF PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) AND/OR SMALL LYMPHOCYTIC LEUKEMIA (SLL)
25MG COPIKTRA SECURA N211155 Sept. 24, 2018 RX CAPSULE ORAL 9840505 Jan. 10, 2032 FOR THE TREATMENT OF PATIENTS WITH FOLLICULAR LYMPHOMA (FL)

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
15MG COPIKTRA SECURA N211155 Sept. 24, 2018 RX CAPSULE ORAL Sept. 24, 2023 NEW CHEMICAL ENTITY
25MG COPIKTRA SECURA N211155 Sept. 24, 2018 RX CAPSULE ORAL Sept. 24, 2023 NEW CHEMICAL ENTITY
15MG COPIKTRA SECURA N211155 Sept. 24, 2018 RX CAPSULE ORAL Sept. 24, 2025 TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) OR SMALL LYMPHOCYTIC LYMPHOMA (SLL) AFTER AT LEAST TWO PRIOR THERAPIES
25MG COPIKTRA SECURA N211155 Sept. 24, 2018 RX CAPSULE ORAL Sept. 24, 2025 TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) OR SMALL LYMPHOCYTIC LYMPHOMA (SLL) AFTER AT LEAST TWO PRIOR THERAPIES

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform Kinase INHIBITOR Kd 10.64 SCIENTIFIC LITERATURE DRUG LABEL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Kinase INHIBITOR Kd 9.62 SCIENTIFIC LITERATURE DRUG LABEL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Kinase INHIBITOR IC50 5.80 IUPHAR
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform Kinase INHIBITOR IC50 7.07 IUPHAR

External reference:

IDSource
610V23S0JI UNII
C4079854 UMLSCUI
CHEMBL3039502 ChEMBL_ID
50905713 PUBCHEM_CID
DB11952 DRUGBANK_ID
D10555 KEGG_DRUG
9856 INN_ID
7795 IUPHAR_LIGAND_ID
017764 NDDF
781354007 SNOMEDCT_US
781364003 SNOMEDCT_US
4037879 VANDF
2058509 RXNORM
289943 MMSL
34993 MMSL
d08900 MMSL
C586691 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Copiktra HUMAN PRESCRIPTION DRUG LABEL 1 71779-115 CAPSULE 15 mg ORAL NDA 27 sections
Copiktra HUMAN PRESCRIPTION DRUG LABEL 1 71779-125 CAPSULE 25 mg ORAL NDA 27 sections
COPIKTRA HUMAN PRESCRIPTION DRUG LABEL 1 73116-215 CAPSULE 15 mg ORAL NDA 26 sections
COPIKTRA HUMAN PRESCRIPTION DRUG LABEL 1 73116-225 CAPSULE 25 mg ORAL NDA 26 sections