General Information of DTT (ID: TTCJG29)

DTT Name Serine/threonine-protein kinase mTOR (mTOR) DTT Info
Gene Name MTOR

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Discontinued Drug(s)
Approved Drug(s)
Clinical Trial Drug(s)
Patented Agent(s)
Investigative Drug(s)
6 Approved Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Everolimus DM8X2EH Advanced cancer 2A00-2F9Z Approved [1]
Novolimus DM6ZPLQ Artery stenosis BD52 Approved [2]
PF-04449913 DMSB068 Chronic myelomonocytic leukaemia 2A40 Approved [3]
Sirolimus DMGW1ID Advanced cancer 2A00-2F9Z Approved [4]
Temsirolimus DMS104F Renal cell carcinoma 2C90 Approved [5]
Zotarolimus DMRMCXW Solid tumour/cancer 2A00-2F9Z Approved [6]
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⏷ Show the Full List of 6 Approved Drug(s)
26 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ridaforolimus DMLHEU7 Sarcoma 2A60-2C35 Phase 3 [7]
ABI-009 DMQ6KZM Malignant perivascular epithelioid cell tumour 2B5Y Phase 2 [8]
AZD2014 DMOEARH Solid tumour/cancer 2A00-2F9Z Phase 2 [9]
BEZ235 DMKBRDL Solid tumour/cancer 2A00-2F9Z Phase 2 [10]
GDC-0980/RG7422 DMF3MV1 Non-hodgkin lymphoma 2B33.5 Phase 2 [2]
INK128 DMGO7QT Breast cancer 2C60-2C65 Phase 2 [11]
LY3023414 DMD9KYF Prostate cancer 2C82.0 Phase 2 [12]
MM-141 DM2RJ4D Pancreatic cancer 2C10 Phase 2 [8]
OSI-027 DMJX3O8 Renal cell carcinoma 2C90 Phase 2 [13]
PF-04691502 DMS610L Endometrial cancer 2C76 Phase 2 [14]
PF-05212384 DMBL3VD Solid tumour/cancer 2A00-2F9Z Phase 2 [15]
PQR309 DMMCYZ8 Squamous head and neck cell carcinom 2D60.0 Phase 2 [2]
Salirasib DMRSU4X Lung cancer 2C25.0 Phase 2 [2]
SAR245409 DMQM7IL Solid tumour/cancer 2A00-2F9Z Phase 2 [2]
SF1126 DML10K3 Head and neck cancer 2D42 Phase 2 [8]
BGT226 DMXKDUL Solid tumour/cancer 2A00-2F9Z Phase 1/2 [16]
CC-223 DMMQYL9 Solid tumour/cancer 2A00-2F9Z Phase 1/2 [17]
ME-344 DM6JN19 Breast cancer 2C60-2C65 Phase 1/2 [18]
BI 860585 DMMQ12N Solid tumour/cancer 2A00-2F9Z Phase 1 [19]
CERC 006 DMM1NGC Lymphatic malformation LA90.1 Phase 1 [20]
DS-3078 DMG7I5J Lymphoma 2A80-2A86 Phase 1 [21]
DS-7423 DMCFJM3 Solid tumour/cancer 2A00-2F9Z Phase 1 [22]
GDC-0349 DM3Z2JB Non-hodgkin lymphoma 2B33.5 Phase 1 [23]
LAM-001 DM7JNHU Lymphangioleiomyomatosis CB07 Phase 1 [24]
PWT-33597 DMJY15D Solid tumour/cancer 2A00-2F9Z Phase 1 [25]
VS-5584 DMMO3G5 Malignant mesothelioma 2C26.0 Phase 1 [2]
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⏷ Show the Full List of 26 Clinical Trial Drug(s)
5 Patented Agent(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
PMID25726713-Compound-47 DMXE5KM N. A. N. A. Patented [26]
PMID25726713-Compound-48 DMSIOUA N. A. N. A. Patented [26]
PMID25726713-Compound-49 DM2CT4G N. A. N. A. Patented [26]
PMID25726713-Compound-50 DM3BDFV N. A. N. A. Patented [26]
PMID25726713-Compound-51 DMF0OW4 N. A. N. A. Patented [26]
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3 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
AZD8055 DM7L8SG Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 1/2 [27]
TAFA-93 DMI52NT Transplant rejection NE84 Discontinued in Phase 1 [28]
SCR-44001 DMFZNUA Solid tumour/cancer 2A00-2F9Z Terminated [29]
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32 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
(4-(6-morpholino-9H-purin-2-yl)phenyl)methanol DMUOFW8 Discovery agent N.A. Investigative [30]
2-(2-Methyl-morpholin-4-yl)-benzo[h]chromen-4-one DMAHZR9 Discovery agent N.A. Investigative [31]
2-(6-morpholino-9H-purin-2-yl)phenol DMZDNHQ Discovery agent N.A. Investigative [30]
2-chloro-N-(6-cyanopyridin-3-yl)propanamide DMBKVM4 Discovery agent N.A. Investigative [32]
2-Morpholin-4-yl-pyrimido[2,1-a]isoquinolin-4-one DM79ZOV Discovery agent N.A. Investigative [31]
3-(6-morpholino-9H-purin-2-yl)phenol DMS2OY9 Discovery agent N.A. Investigative [30]
4-(2-(1H-indol-6-yl)-9H-purin-6-yl)morpholine DMTJGBL Discovery agent N.A. Investigative [30]
4-(2-(thiophen-2-yl)-9H-purin-6-yl)morpholine DMWN1CM Discovery agent N.A. Investigative [30]
4-(2-(thiophen-3-yl)-9H-purin-6-yl)morpholine DMAO6X9 Discovery agent N.A. Investigative [30]
4-(6-morpholino-9H-purin-2-yl)phenol DM1Z3N6 Discovery agent N.A. Investigative [30]
AP-21967 DMCNG74 Discovery agent N.A. Investigative [33]
AR-mTOR-26 DM24MKI Solid tumour/cancer 2A00-2F9Z Investigative [2]
C-16-(S)-3-methylindolerapamycin DMZXE6O Discovery agent N.A. Investigative [33]
CU-906 DMY1WEM Solid tumour/cancer 2A00-2F9Z Investigative [2]
EC-0565 DMIC372 Solid tumour/cancer 2A00-2F9Z Investigative [2]
EC-0845 DMK6E10 Inflammation 1A00-CA43.1 Investigative [2]
EM-101 DMQ63J2 Solid tumour/cancer 2A00-2F9Z Investigative [2]
Ethyl 1-[(1H-benzimidazol-2(3H)one-5-yl)sulfonyl]-1H-pyrrole-2-carboxylate DM3FH02 Discovery agent N.A. Investigative [31]
HM-5016699 DMKHVUE Solid tumour/cancer 2A00-2F9Z Investigative [2]
OXA-01 DMCFM2E Solid tumour/cancer 2A00-2F9Z Investigative [2]
P-2281 DMZI8QW Ulcerative colitis DD71 Investigative [2]
P-6915 DMJDI7O Solid tumour/cancer 2A00-2F9Z Investigative [2]
PF-03772304 DMJ0936 Solid tumour/cancer 2A00-2F9Z Investigative [34]
PF-05094037 DMZAE97 Solid tumour/cancer 2A00-2F9Z Investigative [2]
PP-242 DM2348V Discovery agent N.A. Investigative [35]
PP121 DMU8KTO Discovery agent N.A. Investigative [35]
Rapamycin complexed with immunophilin FKBP12 DMLBP3F Discovery agent N.A. Investigative [36]
SB-2280 DMIBS95 Solid tumour/cancer 2A00-2F9Z Investigative [2]
SX-MTR1 DMJGZ79 Bladder cancer 2C94 Investigative [2]
torin 1 DMZD0NA Discovery agent N.A. Investigative [37]
Torin2 DMC6U93 T-cell leukaemia 2A90 Investigative [38]
X-387 DMZ0TDL Solid tumour/cancer 2A00-2F9Z Investigative [2]
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⏷ Show the Full List of 32 Investigative Drug(s)
Molecule Interaction Atlas

References

1 Mammalian target of rapamycin, its mode of action and clinical response in metastatic clear cell carcinoma. Gan To Kagaku Ryoho. 2009 Jul;36(7):1076-9.
2 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: 2109).
3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4 Knockouts model the 100 best-selling drugs--will they model the next 100 Nat Rev Drug Discov. 2003 Jan;2(1):38-51.
5 Advances in kinase targeting: current clinical use and clinical trials. Trends Pharmacol Sci. 2014 Nov;35(11):604-20.
6 Natural products to drugs: natural product-derived compounds in clinical trials. Nat Prod Rep. 2008 Jun;25(3):475-516.
7 A novel c-Met inhibitor, MK8033, synergizes with carboplatin plus paclitaxel to inhibit ovarian cancer cell growth. Oncol Rep. 2013 May;29(5):2011-8.
8 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
9 Dramatic suppression of colorectal cancer cell growth by the dual mTORC1 and mTORC2 inhibitor AZD-2014. Biochem Biophys Res Commun. 2014 Jan 10;443(2):406-12.
10 The dual PI3K/mTOR inhibitor NVP-BEZ235 is a potent inhibitor of ATM- and DNA-PKCs-mediated DNA damage responses. Neoplasia. 2012 Jan;14(1):34-43.
11 2011 Pipeline of Intellikine.
12 Company report (Lilly)
13 Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov. 2009 Aug;8(8):627-44.
14 PF-04691502, a potent and selective oral inhibitor of PI3K and mTOR kinases with antitumor activity.Mol Cancer Ther.2011 Nov;10(11):2189-99.
15 First-in-Human Study of PF-05212384 (PKI-587), a Small-Molecule, Intravenous, Dual Inhibitor of PI3K and mTOR in Patients with Advanced Cancer. Clin Cancer Res. 2015 Apr 15;21(8):1888-95.
16 Simultaneous targeting of PI3K and mTOR with NVP-BGT226 is highly effective in multiple myeloma. Anticancer Drugs. 2012 Jan;23(1):131-8.
17 CC-223, a Potent and Selective Inhibitor of mTOR Kinase: In Vitro and In Vivo Characterization. Mol Cancer Ther. 2015 Jun;14(6):1295-305.
18 National Cancer Institute Drug Dictionary (drug id 728650).
19 Clinical pipeline report, company report or official report of tatcongress.
20 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2023. Adis Insight
21 A first-in-human Phase I study of DS-3078a, an oral TORC1/2 inhibitor, in patients with advanced solid tumors: Preliminary results, Mol Cancer Ther November,2013, 12, C173.
22 Antitumor activity and induction of TP53-dependent apoptosis toward ovarian clear cell adenocarcinoma by the dual PI3K/mTOR inhibitor DS-7423. PLoS One. 2014 Feb 4;9(2):e87220.
23 Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349. ACS Med Chem Lett. 2012 Nov 29;4(1):103-7.
24 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
25 PIK3CA mutation H1047R is associated with response to PI3K/AKT/mTOR signaling pathway inhibitors in early phase clinical trials
26 Hedgehog inhibitors: a patent review (2013 - present).Expert Opin Ther Pat. 2015 May;25(5):549-65.
27 Clinical pipeline report, company report or official report of AstraZeneca (2009).
28 EP patent application no. 2275103, Mtor inhibitors in the treatment of endocrine tumors.
29 Early detection of response to experimental chemotherapeutic Top216 with [18F]FLT and [18F]FDG PET in human ovary cancer xenografts in mice. PLoS One. 2010 Sep 24;5(9):e12965.
30 Novel purine and pyrazolo[3,4-d]pyrimidine inhibitors of PI3 kinase-alpha: Hit to lead studies. Bioorg Med Chem Lett. 2010 Jan 15;20(2):636-9.
31 Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and... J Med Chem. 2005 Jan 27;48(2):569-85.
32 Synthesis and therapeutic evaluation of pyridyl based novel mTOR inhibitors. Bioorg Med Chem Lett. 2009 Jun 1;19(11):2949-52.
33 The rapamycin-binding domain of the protein kinase mammalian target of rapamycin is a destabilizing domain. J Biol Chem. 2007 May 4;282(18):13395-401.
34 Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design. ACS Med Chem Lett. 2012 Nov 7;4(1):91-7.
35 Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9.
36 Selected novel anticancer treatments targeting cell signaling proteins. Oncologist. 2001;6(6):517-37.
37 Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer. J Med Chem. 2010 Oct 14;53(19):7146-55.
38 Torin2 Potentiates Anticancer Effects on Adult T-Cell Leukemia/Lymphoma by Inhibiting Mammalian Target of Rapamycin. Anticancer Res. 2016 Jan;36(1):95-102.