DGIdb - ADAVOSERTIB Drug Record

ADAVOSERTIB chembl:CHEMBL1976040 Antineoplastic

Alternate Names:

MK-1775
AZD 1775
AZD-1775
ADAVOSERTIB
AZD1775

Drug Info:

FDA Approval	not approved
Drug Class	Small molecule
Drug Indications	antineoplastic agent

(4 More Sources)

Publications:

Sarcar et al., 2011, Targeting radiation-induced G(2) checkpoint activation with the Wee-1 inhibitor MK-1775 in glioblastoma cell lines., Mol. Cancer Ther.
Leijen et al., 2016, Phase I Study Evaluating WEE1 Inhibitor AZD1775 As Monotherapy and in Combination With Gemcitabine, Cisplatin, or Carboplatin in Patients With Advanced Solid Tumors., J. Clin. Oncol.
Lescarbeau et al., 2016, Quantitative Phosphoproteomics Reveals Wee1 Kinase as a Therapeutic Target in a Model of Proneural Glioblastoma., Mol. Cancer Ther.
Bridges et al., 2011, MK-1775, a novel Wee1 kinase inhibitor, radiosensitizes p53-defective human tumor cells., Clin. Cancer Res.
Rajeshkumar et al., 2011, MK-1775, a potent Wee1 inhibitor, synergizes with gemcitabine to achieve tumor regressions, selectively in p53-deficient pancreatic cancer xenografts., Clin. Cancer Res.
Hirai et al., 2009, Small-molecule inhibition of Wee1 kinase by MK-1775 selectively sensitizes p53-deficient tumor cells to DNA-damaging agents., Mol. Cancer Ther.
Richer et al., 2017, WEE1 Kinase Inhibitor AZD1775 Has Preclinical Efficacy in LKB1-Deficient Non-Small Cell Lung Cancer., Cancer Res.
Kreahling et al., 2013, Wee1 inhibition by MK-1775 leads to tumor inhibition and enhances efficacy of gemcitabine in human sarcomas., PLoS ONE
Carrassa et al., 2012, Combined inhibition of Chk1 and Wee1: in vitro synergistic effect translates to tumor growth inhibition in vivo., Cell Cycle
Leijen et al., 2016, Phase II Study of WEE1 Inhibitor AZD1775 Plus Carboplatin in Patients With TP53-Mutated Ovarian Cancer Refractory or Resistant to First-Line Therapy Within 3 Months., J. Clin. Oncol.
Mueller S et al., 2014, Targeting Wee1 for the treatment of pediatric high-grade gliomas., Neuro Oncol
Caretti V et al., 2013, WEE1 kinase inhibition enhances the radiation response of diffuse intrinsic pontine gliomas., Mol Cancer Ther
Weisberg et al., 2015, Identification of Wee1 as a novel therapeutic target for mutant RAS-driven acute leukemia and other malignancies., Leukemia

ADAVOSERTIB WEE1

Interaction Score: 1.71

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serine/threonine-protein kinase WEE1 inhibitor

Notes

PMIDs:
24305702 23270927 19887545

Sources:
TALC TdgClinicalTrial ChemblInteractions CIViC TTD
ADAVOSERTIB TBK1

Interaction Score: 0.27

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ADAVOSERTIB IKBKE

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ADAVOSERTIB STK11

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy MK-1775 + Cisplatin

Indication/Tumor Type non-small cell lung carcinoma

Response Type predicted – sensitive

PMIDs:
28652249

Sources:
JAX-CKB
ADAVOSERTIB NEK2

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ADAVOSERTIB CSNK1A1

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ADAVOSERTIB PRKCQ

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ADAVOSERTIB TYRO3

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ADAVOSERTIB PAK4

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ADAVOSERTIB TNK2

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ADAVOSERTIB NRAS

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type sensitive

PMIDs:
24791855

Sources:
JAX-CKB
ADAVOSERTIB LRRK2

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ADAVOSERTIB PTK2

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ADAVOSERTIB SYK

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ADAVOSERTIB TAOK1

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ADAVOSERTIB JAK3

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ADAVOSERTIB MAP4K5

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ADAVOSERTIB FYN

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ADAVOSERTIB KRAS

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy MK-1775 + Cisplatin

Indication/Tumor Type non-small cell lung carcinoma

Response Type predicted – sensitive

PMIDs:
27998224 24791855 28652249

Sources:
JAX-CKB
ADAVOSERTIB TP53

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

combination therapy MK-1775 + Carboplatin

Indication/Tumor Type ovarian cancer

PMIDs:
21992793 27601554 27196784 21799033 21389100 19887545 28652249 23520471 22713237 27998224

Sources:
JAX-CKB
ADAVOSERTIB PRKD3

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ADAVOSERTIB MAP4K4

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ADAVOSERTIB CDK5

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ADAVOSERTIB BRCA1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Phase II

Response Type predicted – sensitive

PMIDs:
27998224

Sources:
JAX-CKB
ADAVOSERTIB CLK4

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ADAVOSERTIB LCK

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ADAVOSERTIB JAK2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ADAVOSERTIB ABL1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ADAVOSERTIB YES1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

TdgClinicalTrial: MK-1775
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Publications:

JAX-CKB: MK-1775

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Weisberg et al., 2015, Identification of Wee1 as a novel therapeutic target for mutant RAS-driven acute leukemia and other malignancies., Leukemia

Richer et al., 2017, WEE1 Kinase Inhibitor AZD1775 Has Preclinical Efficacy in LKB1-Deficient Non-Small Cell Lung Cancer., Cancer Res.

Leijen et al., 2016, Phase II Study of WEE1 Inhibitor AZD1775 Plus Carboplatin in Patients With TP53-Mutated Ovarian Cancer Refractory or Resistant to First-Line Therapy Within 3 Months., J. Clin. Oncol.

CIViC: ADAVOSERTIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Caretti V et al., 2013, WEE1 kinase inhibition enhances the radiation response of diffuse intrinsic pontine gliomas., Mol Cancer Ther

Mueller S et al., 2014, Targeting Wee1 for the treatment of pediatric high-grade gliomas., Neuro Oncol

TALC: MK-1775
- Version: 12-May-2016
Alternate Names:

MK-1775 Primary Drug Name

MK-1775 Drug Generic Name

Drug Info:

Publications:
DTC: AZD-1775
- Version: 02-September-2020
Alternate Names:

CHEMBL1976040 ChEMBL Drug ID

Drug Info:

Publications:
TTD: MK-1775
- Version: 2020.06.01
Alternate Names:

D02KKA TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL1976040
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL1976040
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Direct Interaction	yes
Mechanism of Interaction	Serine/threonine-protein kinase WEE1 inhibitor
Notes

combination therapy	MK-1775 + Cisplatin
Indication/Tumor Type	non-small cell lung carcinoma
Response Type	predicted – sensitive

Evidence Type	Actionable
Approval Status	Preclinical
Response Type	sensitive

ADAVOSERTIB Drug Record

ADAVOSERTIB chembl:CHEMBL1976040 Antineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Serine/threonine-protein kinase WEE1 inhibitor Notes

PMIDs: 24305702 23270927 19887545

Sources: TALC TdgClinicalTrial ChemblInteractions CIViC TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info: combination therapy MK-1775 + Cisplatin Indication/Tumor Type non-small cell lung carcinoma Response Type predicted – sensitive

PMIDs: 28652249

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info: Evidence Type Actionable Approval Status Preclinical Response Type sensitive

PMIDs: 24791855

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info: combination therapy MK-1775 + Cisplatin Indication/Tumor Type non-small cell lung carcinoma Response Type predicted – sensitive

PMIDs: 27998224 24791855 28652249

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serine/threonine-protein kinase WEE1 inhibitor

Notes

PMIDs:
24305702 23270927 19887545

Sources:
TALC TdgClinicalTrial ChemblInteractions CIViC TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy MK-1775 + Cisplatin

Indication/Tumor Type non-small cell lung carcinoma

Response Type predicted – sensitive

PMIDs:
28652249

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type sensitive

PMIDs:
24791855

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy MK-1775 + Cisplatin

Indication/Tumor Type non-small cell lung carcinoma

Response Type predicted – sensitive

PMIDs:
27998224 24791855 28652249

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

combination therapy MK-1775 + Carboplatin

Indication/Tumor Type ovarian cancer

PMIDs:
21992793 27601554 27196784 21799033 21389100 19887545 28652249 23520471 22713237 27998224

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Phase II

Response Type predicted – sensitive

PMIDs:
27998224

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
None found