General Information of Drug (ID: DM1WEHC)

Drug Name
Buparlisib Drug Info
Synonyms BKM120
Indication
Disease Entry ICD 11 Status REF
Breast cancer 2C60-2C65 Phase 3 [1]
Cross-matching ID
PubChem CID
16654980
ChEBI ID
CHEBI:71954
CAS Number
CAS 944396-07-0
TTD Drug ID
DM1WEHC

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Clinical Trial Drug(s)
Discontinued Drug(s)
Investigative Drug(s)
Approved Drug(s)
Drug(s) Targeting PI3-kinase beta (PIK3CB)
Drug Name Drug ID Indication ICD 11 Highest Status REF
PQR309 DMMCYZ8 Squamous head and neck cell carcinom 2D60.0 Phase 2 [6]
PA-799 DMLSYJQ Colorectal cancer 2B91.Z Phase 1/2 [7]
AZD8186 DMWYF1H Solid tumour/cancer 2A00-2F9Z Phase 1 [8]
GSK2636771 DMCBGLW Prostate cancer 2C82.0 Phase 1 [9]
BAY 1082439 DMLRGX1 Solid tumour/cancer 2A00-2F9Z Phase 1 [10]
AZD6482 DMVP4E5 Thrombosis DB61-GB90 Terminated [11]
PP121 DMU8KTO Discovery agent N.A. Investigative [12]
PIK-75 DM9BQTX Discovery agent N.A. Investigative [13]
KU-0060648 DMQWS6U Discovery agent N.A. Investigative [14]
PI-3065 DMCQUWI Discovery agent N.A. Investigative [15]
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Drug(s) Targeting PI3-kinase delta (PIK3CD)
Drug Name Drug ID Indication ICD 11 Highest Status REF
BAY 80-6946 DMLOS5R Follicular lymphoma 2A80 Approved [16]
Idelalisib DM602WT Chronic lymphocytic leukaemia 2A82.0 Approved [17]
Umbralisib DMYRBO1 Follicular lymphoma 2A80 Approved [18]
IPI-145 DMWA24P Follicular lymphoma 2A80 Approved [19]
Leniolisib DMWAD93 Stomach cancer 2B72 Approved [20]
INCB50465 DMZJP2T Diffuse large B-cell lymphoma 2A81 Phase 2 [21]
ME-401 DMK0UOY Follicular lymphoma 2A80 Phase 2 [21]
RP6530 DMYILGK Chronic lymphocytic leukaemia 2A82.0 Phase 2 [21]
Parsaclisib DMYBIFS Follicular lymphoma 2A80 Phase 2 [22]
AZD8154 DMK13L1 Asthma CA23 Phase 2 [23]
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Drug(s) Targeting PI3-kinase alpha (PIK3CA)
Drug Name Drug ID Indication ICD 11 Highest Status REF
BAY 80-6946 DMLOS5R Follicular lymphoma 2A80 Approved [16]
Alpelisib DMEXMYK Breast cancer 2C60-2C65 Approved [24]
GDC-0032 DMT4QHD Breast cancer 2C60-2C65 Phase 3 [25]
LY3023414 DMD9KYF Prostate cancer 2C82.0 Phase 2 [26]
PA-799 DMLSYJQ Colorectal cancer 2B91.Z Phase 1/2 [7]
MLN1117 DMCVBQD Solid tumour/cancer 2A00-2F9Z Phase 1/2 [27]
PWT-33597 DMJY15D Solid tumour/cancer 2A00-2F9Z Phase 1 [10]
BLY719 DMYHNV3 Solid tumour/cancer 2A00-2F9Z Phase 1 [28]
HHCYH33 DMRQ4L6 Breast cancer 2C60-2C65 Phase 1 [29]
LY3849524 DM8I68X Breast cancer 2C60-2C65 Phase 1 [30]
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Drug(s) Targeting PI3-kinase gamma (PIK3CG)
Drug Name Drug ID Indication ICD 11 Highest Status REF
BAY 80-6946 DMLOS5R Follicular lymphoma 2A80 Approved [31]
IPI-145 DMWA24P Follicular lymphoma 2A80 Approved [19]
Enzastaurin DM5H0R9 Diffuse large B-cell lymphoma 2A81 Phase 3 [21]
Rigosertib DMOSTXF Myelodysplastic syndrome 2A37 Phase 3 [32]
GDC-0032 DMT4QHD Breast cancer 2C60-2C65 Phase 3 [21]
PQR309 DMMCYZ8 Squamous head and neck cell carcinom 2D60.0 Phase 2 [33]
SAR245409 DMQM7IL Solid tumour/cancer 2A00-2F9Z Phase 2 [34]
XL147 DMML7BE Solid tumour/cancer 2A00-2F9Z Phase 2 [34]
SF1126 DML10K3 Head and neck cancer 2D42 Phase 2 [35]
PF-05212384 DMBL3VD Solid tumour/cancer 2A00-2F9Z Phase 2 [36]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [37]
Gefitinib DM15F0X Colon adenocarcinoma Approved [38]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [39]
Selenium DM25CGV N. A. N. A. Approved [40]
Quercetin DM3NC4M Obesity 5B81 Approved [41]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [42]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [43]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [44]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [45]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [46]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [47]
Gefitinib DM15F0X Colon adenocarcinoma Approved [48]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [49]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [50]
Etretinate DM2CZFA Keratosis ED56 Approved [51]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [52]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [53]
Lapatinib DM3BH1Y Breast cancer 2C60-2C65 Approved [54]
Quercetin DM3NC4M Obesity 5B81 Approved [55]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [56]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [57]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [58]
Quercetin DM3NC4M Obesity 5B81 Approved [59]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [60]
Remdesivir DMBFZ6L Coronavirus Disease 2019 (COVID-19) 1D6Y Approved [61]
Acetic Acid, Glacial DM4SJ5Y infection in the ear canal AA0Y Approved [62]
Nefazodone DM4ZS8M Major depressive disorder 6A70.3 Approved [63]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [64]
Leflunomide DMR8ONJ Arthritis FA20 Approved [65]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [66]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Poly polymerase 1 (PARP1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [67]
Gefitinib DM15F0X Colon adenocarcinoma Approved [68]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [69]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [50]
Citalopram DM2G9AE Acute coronary syndrome BA41 Approved [70]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [71]
Imipramine DM2NUH3 Depression 6A70-6A7Z Approved [70]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [72]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [73]
Methotrexate DM2TEOL Anterior urethra cancer Approved [74]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sevoflurane DMC9O43 Anaesthesia 9A78.6 Approved [75]
Docetaxel DMDI269 Advanced cancer 2A00-2F9Z Approved [76]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [77]
Gemcitabine DMSE3I7 Anterior urethra cancer Approved [78]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [79]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [67]
Verapamil DMA7PEW Angina pectoris BA40 Approved [80]
Mechlorethamine DM0CVXA Chronic myelogenous leukaemia 2A20.0 Approved [81]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [82]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [83]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Bosutinib DMTI8YE Blast phase chronic myelogenous leukemia, BCR-ABL1 positive Approved [84]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [85]
Methotrexate DM2TEOL Anterior urethra cancer Approved [86]
Quercetin DM3NC4M Obesity 5B81 Approved [87]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [88]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [89]
Plicamycin DM7C8YV Hypercalcaemia 5B91.0 Approved [90]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [91]
Sevoflurane DMC9O43 Anaesthesia 9A78.6 Approved [91]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [92]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [93]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [94]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [95]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [82]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [96]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [97]
Secobarbital DM14RF5 Epilepsy 8A60-8A68 Approved [98]
Gefitinib DM15F0X Colon adenocarcinoma Approved [99]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [100]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [101]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ethanol DMDRQZU Chronic pain MG30 Approved [102]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [94]
Carvedilol DMHTEAO Chronic heart failure BD1Z Approved [103]
Paclitaxel DMLB81S Breast carcinoma Approved [104]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [105]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [93]
Urokinase DM0GOUD Myocardial infarction BA41-BA43 Approved [79]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [106]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [82]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [96]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [107]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [108]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [109]
Gefitinib DM15F0X Colon adenocarcinoma Approved [110]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [111]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [112]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [113]
Quercetin DM3NC4M Obesity 5B81 Approved [114]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [115]
Hydroquinone DM6AVR4 Melasma ED60.1 Approved [116]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Caspase-3 (CASP3)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sevoflurane DMC9O43 Anaesthesia 9A78.6 Approved [117]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [118]
Lovastatin DM9OZWQ Arteriosclerosis BD40 Approved [119]
Cidofovir DMA13GD Cytomegalovirus infection 1D82 Approved [120]
Docetaxel DMDI269 Advanced cancer 2A00-2F9Z Approved [121]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [122]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [123]
Mannitol DMSCDY9 Bronchiectasis CA24 Approved [124]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [125]
Aprepitant DM053KT Depression 6A70-6A7Z Approved [126]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [127]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [128]
Gefitinib DM15F0X Colon adenocarcinoma Approved [129]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [130]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [131]
Quercetin DM3NC4M Obesity 5B81 Approved [132]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [133]
Glucosamine DM4ZLFD Osteoarthritis FA00-FA05 Approved [134]
Vinblastine DM5TVS3 Advanced cancer 2A00-2F9Z Approved [131]
Ethacrynic acid DM60QMR Edema MG29 Approved [135]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [136]
Methotrexate DM2TEOL Anterior urethra cancer Approved [137]
Crizotinib DM4F29C Non-small-cell lung cancer 2C25.Y Approved [138]
Glucosamine DM4ZLFD Osteoarthritis FA00-FA05 Approved [139]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [140]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [141]
Testosterone DM7HUNW Hot flushes GA30 Approved [142]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [143]
Capivasertib DM9SKW8 Breast cancer 2C60-2C65 Approved [144]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [66]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [82]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [145]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [146]
Methotrexate DM2TEOL Anterior urethra cancer Approved [147]
Dactinomycin DM2YGNW Adult kidney Wilms tumor Approved [148]
Quercetin DM3NC4M Obesity 5B81 Approved [149]
Penicillamine DM40EF6 Cystinuria 5C60.2 Approved [150]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [145]
Glucosamine DM4ZLFD Osteoarthritis FA00-FA05 Approved [151]
Ethacrynic acid DM60QMR Edema MG29 Approved [152]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Paclitaxel DMLB81S Breast carcinoma Approved [153]
Aprepitant DM053KT Depression 6A70-6A7Z Approved [126]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [154]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [50]
Methotrexate DM2TEOL Anterior urethra cancer Approved [155]
obeticholic acid DM3Q1SM Primary biliary cholangitis DB96.1 Approved [156]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [157]
Cyclophosphamide DM4O2Z7 Advanced cancer 2A00-2F9Z Approved [158]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [159]
Trovafloxacin DM6AN32 Acute gonococcal cervicitis Approved [160]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Paclitaxel DMLB81S Breast carcinoma Approved [153]
Aprepitant DM053KT Depression 6A70-6A7Z Approved [126]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [161]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [162]
Crizotinib DM4F29C Non-small-cell lung cancer 2C25.Y Approved [163]
Chlorpromazine DMBGZI3 Acute intermittent hepatic porphyria 5C58.11 Approved [164]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [4]
Trovafloxacin DM6AN32 Acute gonococcal cervicitis Approved [160]
Etodolac DM6WJO9 Osteoarthritis FA00-FA05 Approved [165]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [166]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Paclitaxel DMLB81S Breast carcinoma Approved [167]
Aprepitant DM053KT Depression 6A70-6A7Z Approved [126]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [106]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [168]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [169]
Quercetin DM3NC4M Obesity 5B81 Approved [170]
obeticholic acid DM3Q1SM Primary biliary cholangitis DB96.1 Approved [156]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [171]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [172]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [46]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [101]
Selenium DM25CGV N. A. N. A. Approved [173]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [52]
Quercetin DM3NC4M Obesity 5B81 Approved [174]
Isoniazid DM5JVS3 Latent tuberculosis infection Approved [175]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [159]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [176]
Hydroquinone DM6AVR4 Melasma ED60.1 Approved [177]
Testosterone DM7HUNW Hot flushes GA30 Approved [178]
Olaparib DM8QB1D Ovarian cancer 2C73 Approved [179]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Capivasertib DM9SKW8 Breast cancer 2C60-2C65 Approved [144]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [180]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [181]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [83]
Gefitinib DM15F0X Colon adenocarcinoma Approved [182]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [183]
Imiquimod DM1TMA3 Alopecia areata ED70.2 Approved [184]
Selenium DM25CGV N. A. N. A. Approved [173]
Methimazole DM25FL8 Hyperthyroidism 5A02 Approved [185]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [112]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
PI3-kinase alpha (PIK3CA) TTEUNMR PK3CA_HUMAN Inhibitor [2]
PI3-kinase beta (PIK3CB) TTTHBCA PK3CB_HUMAN Inhibitor [2]
PI3-kinase delta (PIK3CD) TTGBPJE PK3CD_HUMAN Inhibitor [2]
PI3-kinase gamma (PIK3CG) TTHBTOP PK3CG_HUMAN Inhibitor [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Apoptosis regulator Bcl-2 (BCL2) OT9DVHC0 BCL2_HUMAN Gene/Protein Processing [3]
Baculoviral IAP repeat-containing protein 2 (BIRC2) OTFXFREP BIRC2_HUMAN Gene/Protein Processing [3]
Baculoviral IAP repeat-containing protein 3 (BIRC3) OT3E95KB BIRC3_HUMAN Gene/Protein Processing [3]
Baculoviral IAP repeat-containing protein 5 (BIRC5) OTILXZYL BIRC5_HUMAN Gene/Protein Processing [4]
Bcl2-associated agonist of cell death (BAD) OT63ERYM BAD_HUMAN Gene/Protein Processing [3]
Caspase-3 (CASP3) OTIJRBE7 CASP3_HUMAN Gene/Protein Processing [3]
E3 ubiquitin-protein ligase XIAP OT24GP9B XIAP_HUMAN Gene/Protein Processing [3]
Forkhead box protein O3 (FOXO3) OTHXQG4P FOXO3_HUMAN Gene/Protein Processing [4]
Induced myeloid leukemia cell differentiation protein Mcl-1 (MCL1) OT2YYI1A MCL1_HUMAN Gene/Protein Processing [3]
Mitogen-activated protein kinase 1 (MAPK1) OTH85PI5 MK01_HUMAN Post-Translational Modifications [5]

References

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: 7878).
2 Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov. 2009 Aug;8(8):627-44.
3 Inhibition of PI3K signaling pathway enhances the chemosensitivity of APL cells to ATO: Proposing novel therapeutic potential for BKM120. Eur J Pharmacol. 2018 Dec 15;841:10-18. doi: 10.1016/j.ejphar.2018.10.007. Epub 2018 Oct 11.
4 Inhibition of PI3K pathway using BKM120 intensified the chemo-sensitivity of breast cancer cells to arsenic trioxide (ATO). Int J Biochem Cell Biol. 2019 Nov;116:105615. doi: 10.1016/j.biocel.2019.105615. Epub 2019 Sep 17.
5 Combination PI3K/MEK inhibition promotes tumor apoptosis and regression in PIK3CA wild-type, KRAS mutant colorectal cancer. Cancer Lett. 2014 Jun 1;347(2):204-11. doi: 10.1016/j.canlet.2014.02.018. Epub 2014 Feb 24.
6 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. (Target id: 2154).
7 The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations. Clin Cancer Res. 2011 May 15;17(10):3272-81.
8 National Cancer Institute Drug Dictionary (drug id 751594).
9 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: 7967).
10 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
11 Human target validation of phosphoinositide 3-kinase (PI3K)beta: effects on platelets and insulin sensitivity, using AZD6482 a novel PI3Kbeta inhibitor. J Thromb Haemost. 2012 Oct;10(10):2127-36.
12 Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9.
13 Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors. Bioorg Med Chem. 2007 Sep 1;15(17):5837-44.
14 1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity. J Med Chem. 2013 Aug 22;56(16):6386-401.
15 Inactivation of PI(3)K p110delta breaks regulatory T-cell-mediated immune tolerance to cancer. Nature. 2014 Jun 19;510(7505):407-11.
16 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
17 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
18 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2021
19 PI3K-delta and PI3K-gamma inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. Chem Biol. 2013 Nov 21;20(11):1364-74.
20 Effective "activated PI3K syndrome"-targeted therapy with the PI3K inhibitor leniolisib. Blood. 2017 Nov 23;130(21):2307-2316.
21 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
22 Parsaclisib, a potent and highly selective PI3K inhibitor, in patients with relapsed or refractory B-cell malignancies. Blood. 2019 Apr 18;133(16):1742-1752.
23 Discovery of AZD8154, a Dual PI3Kgamma-delta Inhibitor for the Treatment of Asthma. J Med Chem. 2021 Jun 24;64(12):8053-8075.
24 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
25 Company report (BioOncology)
26 Company report (Lilly)
27 National Cancer Institute Drug Dictionary (drug id 714372).
28 In vitro anticancer activity of PI3K alpha selective inhibitor BYL719 in head and neck cancer. Anticancer Res. 2015 Jan;35(1):175-82.
29 Adaptive resistance to PI3Kalpha-selective inhibitor CYH33 is mediated by genomic and transcriptomic alterations in ESCC cells. Cell Death Dis. 2021 Jan 14;12(1):85.
30 ClinicalTrials.gov (NCT05307705) A Study of LOXO-783 Administered as Monotherapy and in Combination With Anticancer Therapies for Patients With Advanced Breast Cancer and Other Solid Tumors With a PIK3CA H1047R Mutation. U.S.National Institutes of Health.
31 BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110 and p110 activities in tumor cell lines and xenograft models.Mol Cancer Ther.2013 Nov;12(11):2319-30.
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