Details of the Drug Combination

General Information of Drug Combination (ID: DCAZI7U)

Drug Combination Name
Letrozole Bicalutamide
Indication
Disease Entry Status REF
Breast Cancer Phase 2 [1]
Component Drugs Letrozole   DMH07Y3 Bicalutamide   DMZMSPF
Small molecular drug Small molecular drug
2D MOL 2D MOL
3D MOL 3D MOL

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of Letrozole
Disease Entry ICD 11 Status REF
Estrogen-receptor positive breast cancer N.A. Approved [2]
Hormonally-responsive breast cancer 2C60-2C65 Approved [3]
Letrozole Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Aromatase (CYP19A1) TTSZLWK CP19A_HUMAN Inhibitor [6]
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Letrozole Interacts with 3 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Metabolism [7]
Aromatase (CYP19A1) DEQX145 CP19A_HUMAN Metabolism [8]
Cytochrome P450 2A6 (CYP2A6) DEJVYAZ CP2A6_HUMAN Metabolism [9]
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Letrozole Interacts with 18 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Aromatase (CYP19A1) OTZ6XF74 CP19A_HUMAN Decreases Activity [10]
Cytochrome P450 3A4 (CYP3A4) OTQGYY83 CP3A4_HUMAN Increases Oxidation [11]
Cytochrome P450 2A6 (CYP2A6) OT52TWG3 CP2A6_HUMAN Increases Oxidation [11]
Adenylate kinase isoenzyme 1 (AK1) OT614AR3 KAD1_HUMAN Increases ADR [12]
Dickkopf-related protein 1 (DKK1) OTRDLUSP DKK1_HUMAN Increases Expression [13]
Follitropin subunit beta (FSHB) OTGLS283 FSHB_HUMAN Increases Expression [14]
Lutropin subunit beta (LHB) OT5GBOVJ LSHB_HUMAN Increases Expression [14]
Progesterone receptor (PGR) OT0FZ3QE PRGR_HUMAN Decreases Expression [15]
Leukemia inhibitory factor (LIF) OTO46S5S LIF_HUMAN Increases Expression [13]
Gap junction alpha-1 protein (GJA1) OTT94MKL CXA1_HUMAN Decreases Expression [16]
G1/S-specific cyclin-D1 (CCND1) OT8HPTKJ CCND1_HUMAN Decreases Expression [17]
G1/S-specific cyclin-D2 (CCND2) OTDULQF9 CCND2_HUMAN Decreases Expression [17]
Cyclin-dependent kinase inhibitor 1 (CDKN1A) OTQWHCZE CDN1A_HUMAN Increases Expression [18]
Leukemia inhibitory factor receptor (LIFR) OT36W9O5 LIFR_HUMAN Increases Expression [13]
Proliferation marker protein Ki-67 (MKI67) OTA8N1QI KI67_HUMAN Decreases Expression [15]
Small ribosomal subunit protein eS6 (RPS6) OTT4D1LN RS6_HUMAN Decreases Phosphorylation [17]
Lanosterol 14-alpha demethylase (CYP51A1) OTAYHG9C CP51A_HUMAN Decreases Activity [19]
Fibroblast growth factor 22 (FGF22) OTVIX6J0 FGF22_HUMAN Increases Expression [13]
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⏷ Show the Full List of 18 DOT(s)
Indication(s) of Bicalutamide
Disease Entry ICD 11 Status REF
Prostate cancer 2C82.0 Approved [4]
Castration-resistant prostate carcinoma N.A. Investigative [5]
Metastatic prostate carcinoma N.A. Investigative [5]
Bicalutamide Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Androgen receptor (AR) TTS64P2 ANDR_HUMAN Antagonist [25]
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Bicalutamide Interacts with 2 DTP Molecule(s)
DTP Name DTP ID UniProt ID Mode of Action REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [26]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [26]
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Bicalutamide Interacts with 1 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Metabolism [27]
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Bicalutamide Interacts with 127 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Androgen receptor (AR) OTUBKAZZ ANDR_HUMAN Decreases Response To Substance [28]
Telomerase reverse transcriptase (TERT) OT085VVA TERT_HUMAN Decreases Expression [20]
Neuropilin-1 (NRP1) OTCGULYV NRP1_HUMAN Decreases Expression [20]
Calmegin (CLGN) OTEWVFQV CLGN_HUMAN Increases Expression [20]
Baculoviral IAP repeat-containing protein 5 (BIRC5) OTILXZYL BIRC5_HUMAN Decreases Expression [20]
Protein regulator of cytokinesis 1 (PRC1) OTHD0XS0 PRC1_HUMAN Decreases Expression [20]
Mitotic checkpoint serine/threonine-protein kinase BUB1 beta (BUB1B) OT8KME51 BUB1B_HUMAN Decreases Expression [20]
H/ACA ribonucleoprotein complex subunit DKC1 (DKC1) OTX7DJR6 DKC1_HUMAN Decreases Expression [20]
Nebulette (NEBL) OT2WH1NC NEBL_HUMAN Increases Expression [20]
Kinesin-like protein KIF20A (KIF20A) OTXOQHE0 KI20A_HUMAN Decreases Expression [20]
Anterior gradient protein 2 homolog (AGR2) OTRRZT7W AGR2_HUMAN Increases Expression [20]
Myc proto-oncogene protein (MYC) OTPV5LUK MYC_HUMAN Decreases Expression [20]
Pro-glucagon (GCG) OTXU08VF GLUC_HUMAN Decreases Expression [20]
Thymidine kinase, cytosolic (TK1) OTY5JFM1 KITH_HUMAN Decreases Expression [20]
Cellular tumor antigen p53 (TP53) OTIE1VH3 P53_HUMAN Increases Expression [20]
Cholinesterase (BCHE) OTOH3WQ9 CHLE_HUMAN Decreases Expression [20]
Cyclin-dependent kinase 1 (CDK1) OTW1SC2N CDK1_HUMAN Decreases Expression [20]
Prostate-specific antigen (KLK3) OTFGSBFJ KLK3_HUMAN Decreases Expression [20]
Amino acid transporter heavy chain SLC3A2 (SLC3A2) OTBR33M9 4F2_HUMAN Increases Expression [20]
Interferon-induced protein with tetratricopeptide repeats 1 (IFIT1) OTXOQDSG IFIT1_HUMAN Decreases Expression [20]
Proliferating cell nuclear antigen (PCNA) OTHZ1RIA PCNA_HUMAN Decreases Expression [20]
Prostatic acid phosphatase (ACP3) OTSIM0YG PPAP_HUMAN Decreases Expression [20]
Cyclic AMP-dependent transcription factor ATF-3 (ATF3) OTC1UOHP ATF3_HUMAN Increases Expression [20]
C-X-C motif chemokine 3 (CXCL3) OTSL94KH CXCL3_HUMAN Increases Expression [20]
Kallikrein-2 (KLK2) OT9RE37R KLK2_HUMAN Decreases Expression [20]
Lamin-B1 (LMNB1) OT100T3P LMNB1_HUMAN Decreases Expression [20]
Midkine (MDK) OTF24HKC MK_HUMAN Increases Expression [20]
Growth arrest and DNA damage-inducible protein GADD45 alpha (GADD45A) OTDRV63V GA45A_HUMAN Increases Expression [20]
Protein S100-P (S100P) OTJCXNJG S100P_HUMAN Increases Expression [20]
Ribonucleoside-diphosphate reductase subunit M2 (RRM2) OTOB6J6R RIR2_HUMAN Decreases Expression [20]
Stress-induced-phosphoprotein 1 (STIP1) OT7TXLOX STIP1_HUMAN Decreases Expression [20]
Cyclin-dependent kinases regulatory subunit 2 (CKS2) OTPTMHIV CKS2_HUMAN Decreases Expression [20]
Mannosyl-oligosaccharide 1,2-alpha-mannosidase IA (MAN1A1) OT6LIGJP MA1A1_HUMAN Increases Expression [20]
Glypican-1 (GPC1) OTQKRSSV GPC1_HUMAN Decreases Expression [20]
Cyclin-dependent kinase inhibitor 1 (CDKN1A) OTQWHCZE CDN1A_HUMAN Increases Expression [20]
Cyclin-dependent kinase 4 inhibitor C (CDKN2C) OTCLOV90 CDN2C_HUMAN Decreases Expression [20]
Ran-specific GTPase-activating protein (RANBP1) OTQE226K RANG_HUMAN Decreases Expression [20]
Proliferation marker protein Ki-67 (MKI67) OTA8N1QI KI67_HUMAN Decreases Expression [20]
DNA replication licensing factor MCM2 (MCM2) OTGGORIQ MCM2_HUMAN Decreases Expression [20]
Aldehyde dehydrogenase family 3 member A2 (ALDH3A2) OT714BUO AL3A2_HUMAN Increases Expression [20]
Serine/threonine-protein kinase Nek2 (NEK2) OT1H27HO NEK2_HUMAN Decreases Expression [20]
Thyroxine 5-deiodinase (DIO3) OTNTITOT IOD3_HUMAN Increases Expression [20]
Neutrophil gelatinase-associated lipocalin (LCN2) OTSB42BR NGAL_HUMAN Increases Expression [20]
Cell division cycle protein 20 homolog (CDC20) OTCOEZRV CDC20_HUMAN Decreases Expression [20]
Mitotic spindle assembly checkpoint protein MAD2A (MAD2L1) OTXNGZCG MD2L1_HUMAN Decreases Expression [20]
Sequestosome-1 (SQSTM1) OTGY5D5J SQSTM_HUMAN Increases Expression [20]
Transmembrane glycoprotein NMB (GPNMB) OTB7KQKV GPNMB_HUMAN Increases Expression [20]
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase (EBP) OTSMGKXQ EBP_HUMAN Decreases Expression [20]
Quinone oxidoreductase PIG3 (TP53I3) OTSCM68G QORX_HUMAN Increases Expression [20]
Retinoic acid-induced protein 3 (GPRC5A) OTPOCWR7 RAI3_HUMAN Decreases Expression [20]
Fibroblast growth factor 13 (FGF13) OTHNNVSG FGF13_HUMAN Increases Expression [20]
Lymphokine-activated killer T-cell-originated protein kinase (PBK) OT5Z27TW TOPK_HUMAN Decreases Expression [20]
Tribbles homolog 3 (TRIB3) OTG5OS7X TRIB3_HUMAN Increases Expression [20]
BRCA1-associated RING domain protein 1 (BARD1) OTTC0Z9Y BARD1_HUMAN Decreases Expression [20]
Homeobox protein Nkx-3.1 (NKX3-1) OT0DO6ZU NKX31_HUMAN Decreases Expression [20]
GTP-binding protein 2 (GTPBP2) OTOJ1KUA GTPB2_HUMAN Increases Expression [20]
Nucleolar and spindle-associated protein 1 (NUSAP1) OT85HIJ5 NUSAP_HUMAN Decreases Expression [20]
Peroxisomal trans-2-enoyl-CoA reductase (PECR) OT5MS8EM PECR_HUMAN Increases Expression [20]
Protein Niban 1 (NIBAN1) OTYOLI12 NIBA1_HUMAN Increases Expression [20]
Rac GTPase-activating protein 1 (RACGAP1) OTQE8IEH RGAP1_HUMAN Decreases Expression [20]
E3 ubiquitin-protein ligase CCNB1IP1 (CCNB1IP1) OTOTVMC8 CIP1_HUMAN Increases Expression [20]
Peptidyl-prolyl cis-trans isomerase FKBP11 (FKBP11) OTY2GC67 FKB11_HUMAN Increases Expression [20]
DnaJ homolog subfamily B member 9 (DNAJB9) OT38EQT6 DNJB9_HUMAN Increases Expression [20]
Alpha-methylacyl-CoA racemase (AMACR) OTUU22PK AMACR_HUMAN Decreases Expression [20]
E3 ISG15--protein ligase HERC5 (HERC5) OTZ5PR39 HERC5_HUMAN Increases Expression [20]
Cell cycle progression protein 1 (CCPG1) OT0IHDKL CCPG1_HUMAN Increases Expression [20]
Targeting protein for Xklp2 (TPX2) OTWLJYH0 TPX2_HUMAN Decreases Expression [20]
Cystine/glutamate transporter (SLC7A11) OTKJ6PXW XCT_HUMAN Increases Expression [20]
Lysosome-associated membrane glycoprotein 3 (LAMP3) OTN0XL3W LAMP3_HUMAN Increases Expression [20]
Hypoxia up-regulated protein 1 (HYOU1) OTBGBSOV HYOU1_HUMAN Increases Expression [20]
Electrogenic sodium bicarbonate cotransporter 1 (SLC4A4) OT727K92 S4A4_HUMAN Decreases Expression [20]
Kunitz-type protease inhibitor 2 (SPINT2) OTQV7BKQ SPIT2_HUMAN Increases Expression [21]
Neprilysin (MME) OT5Q39P8 NEP_HUMAN Increases Expression [21]
Retinoic acid receptor beta (RARB) OT367U3E RARB_HUMAN Increases Expression [21]
S-adenosylmethionine decarboxylase proenzyme (AMD1) OTKAGZY3 DCAM_HUMAN Increases Expression [21]
CD9 antigen (CD9) OT2184XU CD9_HUMAN Increases Expression [21]
Long-chain-fatty-acid--CoA ligase 1 (ACSL1) OTB06ESI ACSL1_HUMAN Increases Expression [21]
Histone H2B type 1-B (H2BC3) OT1BLFJO H2B1B_HUMAN Increases Expression [21]
Lipopolysaccharide-responsive and beige-like anchor protein (LRBA) OTOUZN9G LRBA_HUMAN Increases Expression [21]
Synaptosomal-associated protein 25 (SNAP25) OTUIQ81Q SNP25_HUMAN Increases Expression [21]
Sorbitol dehydrogenase (SORD) OTC44CR6 DHSO_HUMAN Increases Expression [21]
Rod outer segment membrane protein 1 (ROM1) OTE7H0YV ROM1_HUMAN Increases Expression [21]
BCL2/adenovirus E1B 19 kDa protein-interacting protein 3 (BNIP3) OT4SO7J4 BNIP3_HUMAN Increases Expression [21]
Cyclin-G2 (CCNG2) OTII38K2 CCNG2_HUMAN Increases Expression [21]
Unconventional myosin-VI (MYO6) OTJQYRC7 MYO6_HUMAN Increases Expression [21]
Retinoblastoma-associated protein (RB1) OTQJUJMZ RB_HUMAN Increases Phosphorylation [22]
Arginase-1 (ARG1) OTHZITAM ARGI1_HUMAN Decreases Expression [29]
Arginase-2, mitochondrial (ARG2) OTCPI0E8 ARGI2_HUMAN Increases Expression [29]
Arf-GAP with SH3 domain, ANK repeat and PH domain-containing protein 2 (ASAP2) OTGEXULW ASAP2_HUMAN Increases Expression [23]
Bile salt export pump (ABCB11) OTRU7THO ABCBB_HUMAN Decreases Activity [30]
Low-density lipoprotein receptor (LDLR) OTH559LU LDLR_HUMAN Affects Localization [31]
Cytochrome P450 1A1 (CYP1A1) OTE4EFH8 CP1A1_HUMAN Decreases Activity [32]
Insulin-like growth factor I (IGF1) OTIIZR61 IGF1_HUMAN Increases Expression [33]
Beta-2 adrenergic receptor (ADRB2) OTSDOX4Q ADRB2_HUMAN Decreases Expression [34]
Beta-microseminoprotein (MSMB) OTYORAJC MSMB_HUMAN Decreases Expression [35]
Apoptosis regulator Bcl-2 (BCL2) OT9DVHC0 BCL2_HUMAN Increases Expression [36]
Prolactin-inducible protein (PIP) OTH719AH PIP_HUMAN Decreases Expression [37]
Cadherin-1 (CDH1) OTFJMXPM CADH1_HUMAN Affects Localization [31]
Lysosome-associated membrane glycoprotein 2 (LAMP2) OTLUGEJC LAMP2_HUMAN Increases Expression [23]
G2/mitotic-specific cyclin-B1 (CCNB1) OT19S7E5 CCNB1_HUMAN Decreases Expression [38]
Insulin-like growth factor-binding protein 3 (IGFBP3) OTIX63TX IBP3_HUMAN Decreases Expression [33]
Insulin-like growth factor-binding protein 2 (IGFBP2) OTG1P60E IBP2_HUMAN Increases Expression [33]
Cyclin-A2 (CCNA2) OTPHHYZJ CCNA2_HUMAN Decreases Expression [38]
Phosphatidylcholine translocator ABCB4 (ABCB4) OTE6PY83 MDR3_HUMAN Decreases Activity [30]
G1/S-specific cyclin-D1 (CCND1) OT8HPTKJ CCND1_HUMAN Decreases Expression [39]
Retinoic acid receptor RXR-beta (RXRB) OTNPDXG2 RXRB_HUMAN Decreases Expression [36]
Coatomer subunit beta' (COPB2) OT82JIGC COPB2_HUMAN Increases Expression [23]
Cyclin-dependent kinase inhibitor 1B (CDKN1B) OTNY5LLZ CDN1B_HUMAN Increases Expression [36]
ATP synthase subunit e, mitochondrial (ATP5ME) OTADVEE2 ATP5I_HUMAN Increases Expression [23]
Phosphatidylinositol 3,4,5-trisphosphate 3-phosphatase and dual-specificity protein phosphatase PTEN (PTEN) OTOWDUNT PTEN_HUMAN Increases Activity [40]
26S proteasome complex subunit SEM1 (SEM1) OTASLBM1 SEM1_HUMAN Increases Expression [23]
Thymosin beta-4 (TMSB4X) OT9HPLP3 TYB4_HUMAN Increases Expression [41]
Apoptosis regulator BAX (BAX) OTAW0V4V BAX_HUMAN Increases Expression [39]
Bcl-2-like protein 1 (BCL2L1) OTRC5K9O B2CL1_HUMAN Decreases Expression [39]
Peptidyl-prolyl cis-trans isomerase FKBP5 (FKBP5) OT404F9K FKBP5_HUMAN Decreases Expression [39]
Angio-associated migratory cell protein (AAMP) OTZXBSS4 AAMP_HUMAN Increases Expression [23]
Translocating chain-associated membrane protein 1 (TRAM1) OT3I0H8E TRAM1_HUMAN Increases Expression [23]
Cytochrome P450 1B1 (CYP1B1) OTYXFLSD CP1B1_HUMAN Decreases Activity [42]
Phosphatidate cytidylyltransferase, mitochondrial (TAMM41) OTXBJ9W5 TAM41_HUMAN Increases Expression [23]
Cell division control protein 6 homolog (CDC6) OTX93FE7 CDC6_HUMAN Decreases Expression [38]
Cytochrome c oxidase assembly factor 1 homolog (COA1) OTHSX40F COA1_HUMAN Increases Expression [23]
Ankyrin repeat and IBR domain-containing protein 1 (ANKIB1) OTGKB7Y2 AKIB1_HUMAN Increases Expression [23]
Methyl-CpG-binding domain protein 2 (MBD2) OTUQPP0R MBD2_HUMAN Increases Expression [23]
Beta-1,4-galactosyltransferase 6 (B4GALT6) OTBM8F2U B4GT6_HUMAN Increases Expression [23]
BTB/POZ domain-containing protein 3 (BTBD3) OTZ607YT BTBD3_HUMAN Increases Expression [23]
Proliferation-associated protein 2G4 (PA2G4) OT7IG7HT PA2G4_HUMAN Increases Response To Substance [43]
Neurotensin/neuromedin N (NTS) OTPGDNQS NEUT_HUMAN Decreases Response To Substance [44]
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⏷ Show the Full List of 127 DOT(s)

References

1 ClinicalTrials.gov (NCT02910050) Bicalutamide Plus Aromatase Inhibitors in ER(+)/AR(+)/HER2(-) Metastatic Breast Cancer
2 Letrozole FDA Label
3 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: 5209).
4 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: 2863).
5 Bicalutamide FDA Label
6 Aromatase inhibitors--theoretical concept and present experiences in the treatment of endometriosis. Zentralbl Gynakol. 2003 Jul-Aug;125(7-8):247-51.
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39 Niclosamide and Bicalutamide Combination Treatment Overcomes Enzalutamide- and Bicalutamide-Resistant Prostate Cancer. Mol Cancer Ther. 2017 Aug;16(8):1521-1530. doi: 10.1158/1535-7163.MCT-16-0912. Epub 2017 May 12.
40 Conditional expression of PTEN alters the androgen responsiveness of prostate cancer cells. Prostate. 2006 Jul 1;66(10):1114-23. doi: 10.1002/pros.20447.
41 Downregulation of thymosin beta4 expression by androgen in prostate cancer LNCaP cells. J Androl. 2008 Mar-Apr;29(2):207-12. doi: 10.2164/jandrol.107.003608. Epub 2007 Oct 3.
42 Association of CYP1A1 and CYP1B1 inhibition in in vitro assays with drug-induced liver injury. J Toxicol Sci. 2021;46(4):167-176. doi: 10.2131/jts.46.167.
43 The ErbB3-binding protein Ebp1 suppresses androgen receptor-mediated gene transcription and tumorigenesis of prostate cancer cells. Proc Natl Acad Sci U S A. 2005 Jul 12;102(28):9890-5. doi: 10.1073/pnas.0503829102. Epub 2005 Jun 30.
44 A role for neurotensin in bicalutamide resistant prostate cancer cells. Prostate. 2007 Feb 1;67(2):190-202. doi: 10.1002/pros.20518.