Identification

Name
Temsirolimus
Accession Number
DB06287
Type
Small Molecule
Groups
Approved
Description

Temsirolimus is an intravenous drug for the treatment of renal cell carcinoma (RCC), developed by Wyeth Pharmaceuticals and approved by the FDA in late May 2007, and was also approved by the European Medicines Agency (EMEA) on November 2007. It is a derivative of sirolimus and is sold as Torisel.

Structure
Thumb
Synonyms
  • 42-[3-Hydroxy-2-(hydroxymethyl)-2-methylpropanoate]rapamycin
External IDs
CCI-779
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ToriselLiquid25 mgIntravenousPfizer2008-01-11Not applicableCanada
ToriselKit25 mg/1mLWyeth Pharmaceuticals Llc, a Subsidiary of Pfizer Inc.2007-07-01Not applicableUs
ToriselInjection, solution, concentrate30 mgIntravenousPfizer Europe Ma Eeig2007-11-19Not applicableEu
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Gd-temsirolimusSolution25 mgIntravenousGenmed A Division Of Pfizer Canada IncNot applicableNot applicableCanada
TemsirolimusKit25 mg/1mLAccord Healthcare Limited2018-08-13Not applicableUs
International/Other Brands
Torisel
Categories
UNII
624KN6GM2T
CAS number
162635-04-3
Weight
Average: 1030.2871
Monoisotopic: 1029.602485741
Chemical Formula
C56H87NO16
InChI Key
CBPNZQVSJQDFBE-FUXHJELOSA-N
InChI
InChI=1S/C56H87NO16/c1-33-17-13-12-14-18-34(2)45(68-9)29-41-22-20-39(7)56(67,73-41)51(63)52(64)57-24-16-15-19-42(57)53(65)71-46(30-43(60)35(3)26-38(6)49(62)50(70-11)48(61)37(5)25-33)36(4)27-40-21-23-44(47(28-40)69-10)72-54(66)55(8,31-58)32-59/h12-14,17-18,26,33,35-37,39-42,44-47,49-50,58-59,62,67H,15-16,19-25,27-32H2,1-11H3/b14-12+,17-13+,34-18+,38-26+/t33-,35-,36-,37-,39-,40+,41+,42+,44-,45+,46+,47-,49-,50+,56-/m1/s1
IUPAC Name
(1R,2R,4S)-4-[(2R)-2-[(1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-1,18-dihydroxy-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-2,3,10,14,20-pentaoxo-11,36-dioxa-4-azatricyclo[30.3.1.0⁴,⁹]hexatriaconta-16,24,26,28-tetraen-12-yl]propyl]-2-methoxycyclohexyl 3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate
SMILES
OCC(C)(CO)C(=O)O[C@@H]1CC[C@@H](C[C@@H](C)[C@]2([H])CC(=O)[C@H](C)\C=C(C)\[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)\C=C\C=C\C=C(C)\[C@@H](OC)C[C@]3([H])CC[C@@H](C)[C@@](O)(O3)C(=O)C(=O)N3CCCC[C@H]3C(=O)O2)C[C@H]1OC

Pharmacology

Indication

For the treatment of renal cell carcinoma (RCC). Also investigated for use/treatment in breast cancer, lymphoma (unspecified), rheumatoid arthritis, and multiple myeloma.

Associated Conditions
Pharmacodynamics
Not Available
Mechanism of action

Temsirolimus is an inhibitor of mTOR (mammalian target of rapamycin). Temsirolimus binds to an intracellular protein (FKBP-12), and the protein-drug complex inhibits the activity of mTOR that controls cell division. Inhibition of mTOR activity resulted in a G1 growth arrest in treated tumor cells. When mTOR was inhibited, its ability to phosphorylate p70S6k and S6 ribosomal protein, which are downstream of mTOR in the PI3 kinase/AKT pathway was blocked. In in vitro studies using renal cell carcinoma cell lines, temsirolimus inhibited the activity of mTOR and resulted in reduced levels of the hypoxia-inducible factors HIF-1 and HIF-2 alpha, and the vascular endothelial growth factor.

TargetActionsOrganism
ASerine/threonine-protein kinase mTOR
inhibitor
Human
Absorption

Infused intravenous over 30 - 60 minutes. Cmax is typically observed at the end of infusion

Volume of distribution

172 L in whole blood of cancer patients; both temsirolimus and sirolimus are extensive distributed partitioned into formed blood elements

Protein binding

87% bound to plasma proteins in vitro at a concentration of 100 ng/ml

Metabolism

Primarily metabolized by cytochrome P450 3A4 in the human liver. Sirolimus, an equally potent metabolite, is the primary metabolite in humans following IV infusion. Other metabolic pathways observed in in vitro temsirolimus metabolism studies include hydroxylation, reduction and demethylation.

Route of elimination

Excreted predominantly in feces (76%), 4.6% of drug and metabolites recovered in urine. 17% of drug was not recovered by either route following a 14-day sample collection.

Half life

Temsirolimus exhibits a bi-exponential decline in whole blood concentrations and the mean half-lives of temsirolimus and sirolimus were 17.3 hr and 54.6 hr, respectively.

Clearance

16.2 L/h (22%)

Toxicity

Temsirolimus has been administered to patients with cancer in phase 1 and 2 trials with repeated intravenous doses as high as 220 mg/m2. The risk of several serious adverse events, including thrombosis, bowel perforation, interstitial lung disease (ILD), seizure, and psychosis, is increased with doses of temsirolimus greater than 25 mg.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(1S,6R)-3-{[3-(TRIFLUOROMETHYL)-5,6-DIHYDRO[1,2,4]TRIAZOLO[4,3-A]PYRAZIN-7(8H)-YL]CARBONYL}-6-(2,4,5-TRIFLUOROPHENYL)CYCLOHEX-3-EN-1-AMINEThe risk or severity of adverse effects can be increased when (1S,6R)-3-{[3-(TRIFLUOROMETHYL)-5,6-DIHYDRO[1,2,4]TRIAZOLO[4,3-A]PYRAZIN-7(8H)-YL]CARBONYL}-6-(2,4,5-TRIFLUOROPHENYL)CYCLOHEX-3-EN-1-AMINE is combined with Temsirolimus.
1,10-PhenanthrolineThe risk or severity of adverse effects can be increased when 1,10-Phenanthroline is combined with Temsirolimus.
2,4-thiazolidinedioneThe therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Temsirolimus.
3,4-DichloroisocoumarinThe risk or severity of adverse effects can be increased when 3,4-Dichloroisocoumarin is combined with Temsirolimus.
4-(2-Aminoethyl)Benzenesulfonyl FluorideThe risk or severity of adverse effects can be increased when 4-(2-Aminoethyl)Benzenesulfonyl Fluoride is combined with Temsirolimus.
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Temsirolimus.
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Temsirolimus.
AcenocoumarolThe serum concentration of Acenocoumarol can be increased when it is combined with Temsirolimus.
AcetaminophenThe serum concentration of Temsirolimus can be increased when it is combined with Acetaminophen.
AcetazolamideThe metabolism of Temsirolimus can be decreased when combined with Acetazolamide.
Food Interactions
Not Available

References

Synthesis Reference

Kwang-Chung Lee, Ting-Huei Lee, Yen-Shih Tung, Chia-Chen Kao, Tzu-Ai Lee, "Process for preparation of temsirolimus." U.S. Patent US20100249415, issued September 30, 2010.

US20100249415
General References
  1. Boni J, Leister C, Burns J, Cincotta M, Hug B, Moore L: Pharmacokinetic profile of temsirolimus with concomitant administration of cytochrome p450-inducing medications. J Clin Pharmacol. 2007 Nov;47(11):1430-9. Epub 2007 Oct 3. [PubMed:17913896]
External Links
Human Metabolome Database
HMDB0015632
KEGG Drug
D06068
KEGG Compound
C15182
PubChem Compound
23724530
PubChem Substance
99443243
ChemSpider
21468899
BindingDB
50343413
ChEBI
79699
ChEMBL
CHEMBL1201182
Therapeutic Targets Database
DAP001222
PharmGKB
PA164746890
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Temsirolimus
ATC Codes
L01XE09 — Temsirolimus
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
FDA label
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Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedTreatmentCancer, Advanced1
0RecruitingPreventionTumors, Solid1
1Active Not RecruitingTreatmentAdult Solid Neoplasm1
1Active Not RecruitingTreatmentCancer of the Ovary / Cervical Cancers / Endometrial Cancers / Fallopian Tube Cancer / Malignant Peritoneal Neoplasm1
1Active Not RecruitingTreatmentCancer, Advanced3
1Active Not RecruitingTreatmentCancer, Advanced / Tumors, Solid1
1Active Not RecruitingTreatmentCancer, Breast / Colon Neoplasms / Lung Cancers / Malignant Neoplasm of Colon / Melanoma / Neoplasms, Breast / Renal Cancers1
1Active Not RecruitingTreatmentCentral Nervous System / Recurrent Lymphoma / Refractory Lymphomas / Tumors, Solid1
1Active Not RecruitingTreatmentMalignant Lymphomas1
1Active Not RecruitingTreatmentUnspecified Adult Solid Tumor, Protocol Specific1
1CompletedNot AvailableHealthy Volunteers1
1CompletedTreatmentAdult Giant Cell Glioblastoma / Adult Glioblastoma / Adult Gliosarcoma1
1CompletedTreatmentAdult Solid Neoplasm1
1CompletedTreatmentAdult Solid Neoplasm / Lung Carcinoid Tumor / Recurrent Digestive System Neuroendocrine Tumor G1 / Recurrent Uterine Corpus Sarcoma / Renal Cell Carcinoma Recurrent / Stage III Renal Cell Cancer / Stage IIIB Uterine Sarcoma / Stage IIIC Uterine Sarcoma / Stage IV Renal Cell Cancer / Stage IVA Uterine Sarcoma / Stage IVB Uterine Sarcoma1
1CompletedTreatmentAdvanced Cancers1
1CompletedTreatmentAdvanced Solid Tumors1
1CompletedTreatmentBrain and Central Nervous System Tumors / Metastatic Cancers1
1CompletedTreatmentBrain and Central Nervous System Tumors / Metastatic Cancers / Unspecified Adult Solid Tumor, Protocol Specific1
1CompletedTreatmentCancer, Advanced2
1CompletedTreatmentCancer, Breast / Endometrial Cancers / Lung Cancers / Malignant Lymphomas / Renal Cancers / Unspecified Adult Solid Tumor, Protocol Specific1
1CompletedTreatmentCancers1
1CompletedTreatmentCancers / Renal Cell Adenocarcinoma1
1CompletedTreatmentChildhood B Acute Lymphoblastic Leukemia / Childhood T Acute Lymphoblastic Leukemia / Mature T-Cell and NK-Cell Non-Hodgkin Lymphoma / Recurrent Childhood Acute Lymphoblastic Leukemia / Recurrent Childhood Lymphoblastic Lymphoma1
1CompletedTreatmentColorectal Adenocarcinoma / Colorectal Cancers1
1CompletedTreatmentEndometrial Papillary Serous Carcinoma / Recurrent Endometrial Carcinoma / Renal Cell Cancer, Recurrent / Stage III Endometrial Carcinoma / Stage III Renal Cell Cancer / Stage IV Endometrial Carcinoma / Stage IV Renal Cell Cancer / Unspecified Adult Solid Tumor, Protocol Specific1
1CompletedTreatmentExtensive Stage Small Cell Lung Cancer / Hereditary Paraganglioma / Male Breast Cancer / Metastatic Gastrointestinal Carcinoid Tumor / Metastatic Pheochromocytoma / Non-Small Cell Lung Cancer Recurrent / Pancreatic Polypeptide Tumor / Paraganglion neoplasm malignant / Recurrent Breast Cancer / Recurrent Cervical Cancer / Recurrent Endometrial Carcinoma / Recurrent Gastrointestinal Carcinoid Tumor / Recurrent Islet Cell Carcinoma / Recurrent Neuroendocrine Carcinoma of the Skin / Recurrent Ovarian Epithelial Cancer / Recurrent Ovarian Germ Cell Tumor / Recurrent Pheochromocytoma / Recurrent Prostate Cancer / Recurrent Uterine Sarcoma / Refractory Small cell lung cancer / Regional Gastrointestinal Carcinoid Tumor / Regional Pheochromocytoma / Renal Cell Cancer, Recurrent / Stage III Cervical Cancer / Stage III Endometrial Carcinoma / Stage III Neuroendocrine Carcinoma of the Skin / Stage III Ovarian Epithelial Cancer / Stage III Ovarian Germ Cell Tumor / Stage III Prostate Cancer / Stage III Renal Cell Cancer / Stage III Uterine Sarcoma / Stage IIIA Breast Cancer / Stage IIIA Non-Small Cell Lung Cancer / Stage IIIB Breast Cancer / Stage IIIb Non-small Cell Lung Cancer / Stage IIIC Breast Cancer / Stage IV Breast Cancer / Stage IV Endometrial Carcinoma / Stage IV Neuroendocrine Carcinoma of the Skin / Stage IV Non-Small Cell Lung Cancer / Stage IV Ovarian Epithelial Cancer / Stage IV Ovarian Germ Cell Tumor / Stage IV Prostate Cancer / Stage IV Renal Cell Cancer / Stage IV Uterine Sarcoma / Stage IVA Cervical Cancer / Stage IVB Cervical Cancer / Thyroid Gland Medullary Carcinoma1
1CompletedTreatmentGenital Neoplasms, Female1
1CompletedTreatmentHepatic Complications / Malignant Lymphomas / Unspecified Adult Solid Tumor, Protocol Specific1
1CompletedTreatmentHepatocellular,Carcinoma1
1CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1CompletedTreatmentMalignant Carcinoma / Neoplasms1
1CompletedTreatmentMelanoma / Recurrent Melanoma / Stage III Melanoma / Stage IV Melanoma1
1CompletedTreatmentNeoplasms, Malignant1
1CompletedTreatmentOvarian Sarcoma / Ovarian Stromal Cancer / Recurrent Endometrial Carcinoma / Recurrent Ovarian Epithelial Cancer / Recurrent Ovarian Germ Cell Tumor / Stage III Endometrial Carcinoma / Stage III Ovarian Epithelial Cancer / Stage III Ovarian Germ Cell Tumor / Stage IV Endometrial Carcinoma / Stage IV Ovarian Epithelial Cancer / Stage IV Ovarian Germ Cell Tumor / Unspecified Adult Solid Tumor, Protocol Specific1
1CompletedTreatmentPediatric Solid Tumors1
1CompletedTreatmentRecurrent Adult Hodgkin's Lymphoma1
1CompletedTreatmentRecurrent Melanoma / Renal Cell Cancer, Recurrent / Stage IV Melanoma / Stage IV Renal Cell Cancer / Unspecified Adult Solid Tumor, Protocol Specific1
1CompletedTreatmentRefractory Follicular Lymphoma1
1CompletedTreatmentRefractory Multiple Myeloma / Stage I Multiple Myeloma / Stage II Multiple Myeloma / Stage III Multiple Myeloma1
1CompletedTreatmentRefractory Multiple Myeloma / Stage II Multiple Myeloma / Stage III Multiple Myeloma1
1CompletedTreatmentRenal Cancers1
1CompletedTreatmentRenal Cancers / Renal Cell Adenocarcinoma1
1CompletedTreatmentRenal Cell Adenocarcinoma1
1CompletedTreatmentResistant Solid Malignancies2
1CompletedTreatmentTriple Negative Breast Cancer (TNBC)1
1CompletedTreatmentTumors, Solid2
1CompletedTreatmentUnspecified Adult Solid Tumor, Protocol Specific2
1CompletedTreatmentUnspecified Childhood Solid Tumor, Protocol Specific2
1Not Yet RecruitingTreatmentLiver Cancer1
1RecruitingTreatmentAdvanced Cancers1
1RecruitingTreatmentAdvanced Cancers / Advanced Malignant Neoplasm / Castleman's Disease / Digestive System Carcinoma / Erdheim-Chester Disease (ECD) / Lip and Oral Cavity Carcinoma / Lymphangioleiomyomatosis / Malignant Endocrine Neoplasm / Malignant Female Reproductive System Neoplasm / Malignant Male Reproductive System Neoplasm / Malignant respiratory tract neoplasm / Malignant Thoracic Neoplasm / Malignant Urinary System Neoplasm / Mesothelial Neoplasm / Metastatic Malignant Neoplasm / Neoplasms, Malignant / Neurofibromatosis Type 2 / Recurrent Adult Soft Tissue Sarcoma / Recurrent Breast Carcinoma / Recurrent Childhood Soft Tissue Sarcoma / Recurrent Digestive System Carcinoma / Recurrent Female Reproductive System Carcinoma / Recurrent Male Reproductive System Carcinoma / Recurrent Malignant Neoplasm / Recurrent Pharyngeal Carcinoma / Recurrent Thyroid Gland Carcinoma / Refractory Malignant Neoplasm / Soft Tissue Neoplasms / Stage III Breast Cancer AJCC V7 / Stage III Pharyngeal Cancer / Stage IIIA Breast Cancer AJCC v7 / Stage IIIB Breast Cancer AJCC v7 / Stage IIIC Breast Cancer AJCC v7 / Stage IV Breast Cancer AJCC v6 and v7 / Stage IV Pharyngeal Cancer / Stage IVA Pharyngeal Cancer / Stage IVB Pharyngeal Cancer / Stage IVC Pharyngeal Cancer / Thyroid Gland Neoplasm / Urothelial carcinoma ureter metastatic1
1RecruitingTreatmentDiffuse Intrinsic Pontine Glioma (DIPG)1
1RecruitingTreatmentLymphoblastic Leukemia, Acute, Childhood / Lymphoma, Lymphoblastic / Peripheral T-Cell Lymphoma (PTCL)1
1RecruitingTreatmentPatients With Advanced or Metastatic Solid Tumors1
1RecruitingTreatmentTumors, Solid1
1TerminatedTreatmentAccelerated Phase Chronic Myelogenous Leukemia / Blastic Phase Chronic Myelogenous Leukemia / Chronic Myelogenous Leukemia, BCR-ABL1 Positive / Chronic Phase Chronic Myelogenous Leukemia / Relapsing Chronic Myelogenous Leukemia1
1TerminatedTreatmentAdenocarcinoma of the Pancreas1
1TerminatedTreatmentAdenocarcinoma of the Prostate / Hormone-Resistant Prostate Cancer / Prostate Cancer / Recurrent Prostate Cancer / Stage IV Prostate Cancer1
1TerminatedTreatmentAdenocarcinoma of the Prostate / Recurrent Prostate Cancer1
1TerminatedTreatmentAdvanced Solid Tumors1
1TerminatedTreatmentBrain and Central Nervous System Tumors / Neuroblastomas / Sarcomas / Unspecified Childhood Solid Tumor, Protocol Specific1
1Unknown StatusTreatmentAdvanced/Recurrent Breast Cancer / Cancer of the Ovary / Endometrial Cancers1
1WithdrawnBasic ScienceNeoplasms, Brain1
1WithdrawnTreatmentGliomas / Neoplasms, Brain Stem / Pinealoma1
1WithdrawnTreatmentUnspecified Adult Solid Tumor, Protocol Specific1
1, 2Active Not RecruitingTreatmentAIDS-Related Hodgkin Lymphoma / Recurrent Adult Diffuse Large Cell Lymphoma / Recurrent Adult Hodgkin's Lymphoma / Recurrent Follicular Lymphoma / Recurrent Lymphoplasmacytic Lymphoma / Recurrent Marginal Zone Lymphoma / Recurrent Non-Hodgkin Lymphoma / Recurrent T-Cell Non-Hodgkin Lymphoma / Waldenström's Macroglobulinemia (WM)1
1, 2Active Not RecruitingTreatmentCognitive Side Effects of Cancer Therapy / Neurotoxicity Syndrome / Recurrent Grade 1 Follicular Lymphoma / Recurrent Grade 2 Follicular Lymphoma / Recurrent Grade 3 Follicular Lymphoma / Recurrent Mantle Cell Lymphoma / Recurrent Marginal Zone Lymphoma / Recurrent Small Lymphocytic Lymphoma / Therapy-Related Toxicity / Tiredness / Waldenström's Macroglobulinemia (WM)1
1, 2CompletedTreatmentAdenocarcinoma, Prostate / Hormone-Resistant Prostate Cancer / Recurrent Prostate Carcinoma / Stage IV Prostate Cancer1
1, 2CompletedTreatmentAdenocarcinomas / Neoplasms1
1, 2CompletedTreatmentAdult Anaplastic Astrocytoma / Adult Anaplastic Oligodendroglioma / Adult Diffuse Astrocytoma / Adult Giant Cell Glioblastoma / Adult Glioblastoma / Adult Gliosarcoma / Adult Mixed Glioma / Adult Pilocytic Astrocytoma / Adult Pineal Gland Astrocytoma / Adult Subependymal Giant Cell Astrocytoma / Recurrent Adult Brain Tumor1
1, 2CompletedTreatmentAdult Giant Cell Glioblastoma / Adult Glioblastoma / Adult Gliosarcoma / Recurrent Adult Brain Neoplasm / Recurrent Adult Brain Tumor1
1, 2CompletedTreatmentAdult Giant Cell Glioblastoma / Adult Glioblastoma / Adult Gliosarcoma / Recurrent Adult Brain Tumor1
1, 2CompletedTreatmentBladder Cancers / Transitional Cell Cancer of the Renal Pelvis and Ureter / Urethral Cancer1
1, 2CompletedTreatmentBrain and Central Nervous System Tumors1
1, 2CompletedTreatmentCancer, Breast1
1, 2CompletedTreatmentClear Cell Renal Cell Carcinoma / Renal Cell Cancer, Recurrent / Stage IV Renal Cell Cancer1
1, 2CompletedTreatmentFollicular Lymphoma (FL) / Mantle Cell Lymphoma (MCL)1
1, 2CompletedTreatmentInoperable HCC1
1, 2CompletedTreatmentMale Breast Cancer / Male Breast Carcinoma / Recurrent Breast Cancer / Recurrent Breast Carcinoma / Stage IV Breast Cancer / Stage IV Breast Cancer AJCC v6 and v71
1, 2CompletedTreatmentMultiple Myeloma (MM)1
1, 2CompletedTreatmentProstate Cancer1
1, 2CompletedTreatmentProstatic Neoplasms1
1, 2CompletedTreatmentRefractory Mantle Cell Lymphoma1
1, 2CompletedTreatmentSarcomas1
1, 2RecruitingTreatmentGlioblastoma, Adult1
1, 2TerminatedTreatmentAdult Anaplastic Astrocytoma / Adult Anaplastic Oligodendroglioma / Adult Diffuse Astrocytoma / Adult Giant Cell Glioblastoma / Adult Glioblastoma / Adult Gliosarcoma / Adult Mixed Glioma / Adult Oligodendroglioma / Recurrent Adult Brain Neoplasm1
1, 2TerminatedTreatmentAdvanced Cancers1
1, 2TerminatedTreatmentAndrogen-insensitive Prostate Cancer / Castrate-resistant Prostate Cancer (CRPC) / Hormone-Refractory Prostate Cancer / Metastatic Disease / Prostate Cancer / Prostatic Neoplasms1
1, 2TerminatedTreatmentCancer, Advanced / Carcinoma, Colorectal / Endometrial / Lung Cancer Non-Small Cell Cancer (NSCLC) / Malignant Neoplasm of Pancreas / Renal Cell Adenocarcinoma / Uterine1
1, 2TerminatedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1, 2TerminatedTreatmentSquamous Cell Carcinoma of the Head and Neck (SCCHN)1
1, 2WithdrawnTreatmentHepatocellular,Carcinoma1
1, 2WithdrawnTreatmentMantle Cell Lymphoma (MCL)1
2Active Not RecruitingTreatmentAdvanced Rare Tumours1
2Active Not RecruitingTreatmentAnaplastic Astrocytoma (AA) / Anaplastic Oligodendroglioma (AO) / Glioblastomas / Mixed Gliomas / Recurrent Brain Tumors1
2Active Not RecruitingTreatmentClear Cell Renal Cell Carcinoma / Renal Cell Cancer, Recurrent / Renal Cell Carcinoma Recurrent / Stage IV Renal Cell Cancer / Stage IV Renal Cell Cancer AJCC V71
2Active Not RecruitingTreatmentDesmoplastic Small Round Cell Tumor (DSRCT) / Ewing Sarcoma of Bone or Soft Tissue / Localized Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor / Metastatic Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor1
2Active Not RecruitingTreatmentEndometrial Adenocarcinomas / Endometrial Adenosquamous Carcinoma / Endometrial Clear Cell Adenocarcinoma / Endometrial Serous Adenocarcinoma / Recurrent Uterine Corpus Carcinoma / Stage IIIA Uterine Corpus Cancer / Stage IIIB Uterine Corpus Cancer / Stage IIIC Uterine Corpus Cancer / Stage IVA Uterine Corpus Cancer / Stage IVB Uterine Corpus Cancer1
2Active Not RecruitingTreatmentEstrogen Receptor Positive / HER2/Neu Positive / Male Breast Carcinoma / Progesterone Receptor Positive / Recurrent Breast Carcinoma / Stage III Breast Cancer AJCC V7 / Stage IIIA Breast Cancer / Stage IIIA Breast Cancer AJCC v7 / Stage IIIB Breast Cancer / Stage IIIB Breast Cancer AJCC v7 / Stage IIIC Breast Cancer / Stage IIIC Breast Cancer AJCC v7 / Stage IV Breast Cancer / Stage IV Breast Cancer AJCC v6 and v71
2Active Not RecruitingTreatmentHepatocellular,Carcinoma1
2Active Not RecruitingTreatmentLymphoma, Large B-Cell, Diffuse (DLBCL)1
2Active Not RecruitingTreatmentMetastatic Cancers1
2Active Not RecruitingTreatmentMetastatic Renal Cell Carcinoma1
2Active Not RecruitingTreatmentRenal Cancers1
2CompletedNot AvailableEndometrioid Carcinoma / MTor Protein1
2CompletedTreatmentAdenocarcinoma of the Cervix / Adenosquamous carcinoma of the cervix / Cervical Squamous Cell Carcinoma / Recurrent Cervical Carcinoma / Stage IIIA Cervical Cancer / Stage IIIB Cervical Cancer / Stage IVA Cervical Cancer / Stage IVB Cervical Cancer1
2CompletedTreatmentAdenocarcinoma of the Pancreas / Recurrent Pancreatic Cancer / Stage II Pancreatic Cancer / Stage III Pancreatic Cancer / Stage IV Pancreatic Cancer1
2CompletedTreatmentAdult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities / Adult Acute Myeloid Leukemia With Inv(16)(p13;q22) / Adult Acute Myeloid Leukemia With T(15;17)(q22;q12) / Adult Acute Myeloid Leukemia With T(16;16)(p13;q22) / Adult Acute Myeloid Leukemia With T(8;21)(q22;q22) / Blastic Phase Chronic Myelogenous Leukemia / Chronic Myelomonocytic Leukemia / De Novo Myelodysplastic Syndromes / Previously Treated Myelodysplastic Syndromes / Recurrent Adult Acute Lymphoblastic Leukemia / Recurrent Adult Acute Myeloid Leukemia / Refractory Anemia With Excess Blasts / Refractory Anemia With Excess Blasts in Transformation / Relapsing Chronic Myelogenous Leukemia / Secondary Myelodysplastic Syndromes1
2CompletedTreatmentAdult Giant Cell Glioblastoma / Adult Glioblastoma / Adult Gliosarcoma / Recurrent Adult Brain Tumor1
2CompletedTreatmentAdult Hepatocellular Carcinoma / Advanced Adult Hepatocellular Carcinoma / Endometrial Serous Adenocarcinoma / Localized Non-Resectable Adult Liver Carcinoma / Lung Carcinoid Tumor / Malignant Ovarian Mixed Epithelial Tumor / Malignant Pancreatic Gastrinoma / Malignant Pancreatic Glucagonoma / Malignant Pancreatic Insulinoma / Malignant Pancreatic Somatostatinoma / Metastatic Digestive System Neuroendocrine Tumor G1 / Ovarian Carcinosarcoma / Ovarian Endometrioid Adenocarcinoma / Ovarian Seromucinous Carcinoma / Ovarian Serous Surface Papillary Adenocarcinoma / Pancreatic Alpha Cell Adenoma / Pancreatic Beta Cell Adenoma / Pancreatic Delta Cell Adenoma / Pancreatic G-Cell Adenoma / Pancreatic Polypeptide Tumor / Recurrent Adult Liver Carcinoma / Recurrent Digestive System Neuroendocrine Tumor G1 / Recurrent Fallopian Tube Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Pancreatic Neuroendocrine Carcinoma / Recurrent Primary Peritoneal Carcinoma / Recurrent Uterine Corpus Carcinoma / Regional Digestive System Neuroendocrine Tumor G1 / Stage IIIA Fallopian Tube Cancer / Stage IIIA Ovarian Cancer / Stage IIIA Primary Peritoneal Cancer / Stage IIIA Uterine Corpus Cancer / Stage IIIB Fallopian Tube Cancer / Stage IIIB Ovarian Cancer / Stage IIIB Primary Peritoneal Cancer / Stage IIIB Uterine Corpus Cancer / Stage IIIC Fallopian Tube Cancer / Stage IIIC Ovarian Cancer / Stage IIIC Primary Peritoneal Cancer / Stage IIIC Uterine Corpus Cancer / Stage IV Fallopian Tube Cancer / Stage IV Ovarian Cancer / Stage IV Primary Peritoneal Cancer / Stage IVA Uterine Corpus Cancer / Stage IVB Uterine Corpus Cancer / Uterine Carcinosarcoma1
2CompletedTreatmentAdult Rhabdomyosarcoma / Childhood Alveolar Rhabdomyosarcoma / Childhood Pleomorphic Rhabdomyosarcoma / Childhood Rhabdomyosarcoma With Mixed Embryonal and Alveolar Features / Previously Treated Childhood Rhabdomyosarcoma / Recurrent Adult Soft Tissue Sarcoma / Recurrent Childhood Rhabdomyosarcoma1
2CompletedTreatmentAdvanced Renal Cell Carcinoma1
2CompletedTreatmentB-Cell Chronic Lymphocytic Leukemia / Chronic Lymphocytic Leukemia (CLL) - Refractory / Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue / Neoplasms, Malignant / Nodal marginal zone B-cell lymphomas / Recurrent Adult Burkitt Lymphoma / Recurrent Adult Diffuse Large Cell Lymphoma / Recurrent Adult Diffuse Mixed Cell Lymphoma / Recurrent Adult Diffuse Small Cleaved Cell Lymphoma / Recurrent Adult Immunoblastic Large Cell Lymphoma / Recurrent Adult Lymphoblastic Lymphoma / Recurrent Grade 1 Follicular Lymphoma / Recurrent Grade 2 Follicular Lymphoma / Recurrent Grade 3 Follicular Lymphoma / Recurrent Marginal Zone Lymphoma / Recurrent Small Lymphocytic Lymphoma / Splenic Marginal Zone Lymphoma / Waldenström's Macroglobulinemia (WM)1
2CompletedTreatmentBrain and Central Nervous System Tumors1
2CompletedTreatmentChildhood Alveolar Soft Part Sarcoma / Childhood Alveolar Soft-part Sarcoma / Childhood Angiosarcoma / Childhood Epithelioid Sarcoma / Childhood Fibrosarcoma / Childhood Gliosarcoma / Childhood Leiomyosarcoma / Childhood Liposarcoma / Childhood Malignant Peripheral Nerve Sheath Tumor / Childhood Neurofibrosarcoma / Childhood Synovial Sarcoma / Previously Treated Childhood Rhabdomyosarcoma / Recurrent Childhood Rhabdomyosarcoma / Recurrent Childhood Soft Tissue Sarcoma / Recurrent Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor / Recurrent Osteosarcoma / Rhabdomyosarcomas1
2CompletedTreatmentEndometrial Adenocarcinomas / Endometrial Adenosquamous Cell Carcinoma / Endometrial Clear Cell Carcinoma / Endometrial Papillary Serous Carcinoma / Recurrent Endometrial Carcinoma / Stage IIIA Endometrial Carcinoma / Stage IIIB Endometrial Carcinoma / Stage IIIC Endometrial Carcinoma / Stage IVA Endometrial Carcinoma / Stage IVB Endometrial Carcinoma1
2CompletedTreatmentEndometrial Carcinoma / Recurrent Uterine Corpus Carcinoma / Stage IIIA Uterine Corpus Cancer / Stage IIIB Uterine Corpus Cancer / Stage IIIC1 Uterine Corpus Cancer / Stage IIIC2 Uterine Corpus Cancer / Stage IVA Uterine Corpus Cancer / Stage IVB Uterine Corpus Cancer1
2CompletedTreatmentExtensive Stage Small Cell Lung Cancer1
2CompletedTreatmentFallopian Tube Cancer / Primary Peritoneal Cavity Cancer / Recurrent Ovarian Epithelial Cancer1
2CompletedTreatmentGanglioneuroblastoma / Recurrent Neuroblastoma1
2CompletedTreatmentGastrointestinal Stromal Tumors / Recurrent Adult Soft Tissue Sarcoma / Stage I Adult Soft Tissue Sarcoma / Stage II Adult Soft Tissue Sarcoma / Stage III Adult Soft Tissue Sarcoma / Stage IV Adult Soft Tissue Sarcoma1
2CompletedTreatmentGenital Diseases, Female / Neoplasms, Endometrial / Neoplasms, Ovarian / Ovarian Diseases1
2CompletedTreatmentGlioblastoma Multiforme (GBM)1
2CompletedTreatmentHER2-mutant Non-Small Cell Lung Cancer1
2CompletedTreatmentHead and Neck Squamous Cell Carcinoma (HNSCC)1
2CompletedTreatmentLeukemias1
2CompletedTreatmentMelanoma (Skin)1
2CompletedTreatmentMetastatic Bone Sarcomas / Recurrent Adult Soft Tissue Sarcoma / Recurrent Osteosarcoma / Stage III Adult Soft Tissue Sarcoma / Stage IV Adult Soft Tissue Sarcoma1
2CompletedTreatmentMetastatic Colorectal Cancers1
2CompletedTreatmentMetastatic Gastrointestinal Carcinoid Tumor / Pulmonary Carcinoid Tumor / Recurrent Gastrointestinal Carcinoid Tumor / Recurrent Islet Cell Carcinoma1
2CompletedTreatmentMetastatic Renal Cell Carcinoma1
2CompletedTreatmentNeoplasms, Breast1
2CompletedTreatmentNon-Hodgkin's Lymphoma (NHL)1
2CompletedTreatmentNon-Small Cell Lung Cancer Recurrent / Stage IIIb Non-small Cell Lung Cancer / Stage IV Non-Small Cell Lung Cancer1
2CompletedTreatmentNon-clear Cell Renal Cell Cancer1
2CompletedTreatmentOvarian Clear Cell Cystadenocarcinoma / Stage III Ovarian Cancer / Stage IV Ovarian Cancer1
2CompletedTreatmentProstate Cancer3
2CompletedTreatmentRecurrent Adult Soft Tissue Sarcoma / Stage III Adult Soft Tissue Sarcoma / Stage IV Adult Soft Tissue Sarcoma1
2CompletedTreatmentRecurrent Endometrial Carcinoma1
2CompletedTreatmentRecurrent Hypopharyngeal Squamous Cell Carcinoma / Recurrent Laryngeal Squamous Cell Carcinoma / Recurrent Laryngeal Verrucous Carcinoma / Recurrent Lip and Oral Cavity Squamous Cell Carcinoma / Recurrent Metastatic Squamous Cell Carcinoma in the Neck With Occult Primary / Recurrent Nasal Cavity and Paranasal Sinus Squamous Cell Carcinoma / Recurrent Nasopharyngeal Keratinizing Squamous Cell Carcinoma / Recurrent Oral Cavity Verrucous Carcinoma / Recurrent Oropharyngeal Squamous Cell Carcinoma / Recurrent Salivary Gland Carcinoma / Salivary Gland Squamous Cell Carcinoma / Squamous Cell Carcinoma Metastatic in the Neck With Occult Primary / Stage IV Hypopharyngeal Squamous Cell Carcinoma / Stage IV Nasopharyngeal Keratinizing Squamous Cell Carcinoma / Stage IVA Laryngeal Squamous Cell Carcinoma / Stage IVA Laryngeal Verrucous Carcinoma / Stage IVA Lip and Oral Cavity Squamous Cell Carcinoma / Stage IVA Major Salivary Gland Carcinoma / Stage IVA Nasal Cavity and Paranasal Sinus Squamous Cell Carcinoma / Stage IVA Oral Cavity Verrucous Carcinoma / Stage IVA Oropharyngeal Squamous Cell Carcinoma / Stage IVB Laryngeal Squamous Cell Carcinoma / Stage IVB Laryngeal Verrucous Carcinoma / Stage IVB Lip and Oral Cavity Squamous Cell Carcinoma / Stage IVB Major Salivary Gland Carcinoma / Stage IVB Nasal Cavity and Paranasal Sinus Squamous Cell Carcinoma / Stage IVB Oral Cavity Verrucous Carcinoma / Stage IVB Oropharyngeal Squamous Cell Carcinoma / Stage IVC Laryngeal Squamous Cell Carcinoma / Stage IVC Laryngeal Verrucous Carcinoma / Stage IVC Lip and Oral Cavity Squamous Cell Carcinoma / Stage IVC Major Salivary Gland Carcinoma / Stage IVC Nasal Cavity and Paranasal Sinus Squamous Cell Carcinoma / Stage IVC Oral Cavity Verrucous Carcinoma / Stage IVC Oropharyngeal Squamous Cell Carcinoma / Tongue Carcinoma1
2CompletedTreatmentRecurrent Mantle Cell Lymphoma2
2CompletedTreatmentRecurrent Melanoma / Stage IIIA Skin Melanoma / Stage IIIB Skin Melanoma / Stage IIIC Skin Melanoma / Stage IV Skin Melanoma1
2CompletedTreatmentRecurrent Melanoma / Stage IV Melanoma1
2CompletedTreatmentRefractory Multiple Myeloma / Stage I Multiple Myeloma / Stage II Multiple Myeloma / Stage III Multiple Myeloma1
2CompletedTreatmentRelapsed Bladder Cancer1
2CompletedTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
2CompletedTreatmentRenal Cancers / Renal Cell Adenocarcinoma1
2CompletedTreatmentThyroid Cancers1
2RecruitingTreatmentAcute Myeloblastic Leukemia1
2RecruitingTreatmentAdvanced Solid Tumors / Multiple Myeloma (MM) / Non-Hodgkin's Lymphoma (NHL)2
2RecruitingTreatmentChronic Limb Ischemia1
2TerminatedTreatmentCancer of the Ovary1
2TerminatedTreatmentChronic Lymphocytic Leukemia (CLL) - Refractory / Recurrent Adult Diffuse Large Cell Lymphoma / Recurrent Adult Hodgkin's Lymphoma1
2TerminatedTreatmentLiver Cancer1
2TerminatedTreatmentMucosal Melanoma / Recurrent Melanoma / Stage IV Melanoma1
2TerminatedTreatmentMyelodysplastic Syndrome1
2TerminatedTreatmentNeuroblastomas1
2TerminatedTreatmentProstate Cancer1
2TerminatedTreatmentRecurrent Uterine Sarcoma / Uterine Carcinosarcoma1
2TerminatedTreatmentRenal Cancers1
2TerminatedTreatmentRenal Cell Adenocarcinoma1
2TerminatedTreatmentRheumatoid Arthritis1
2TerminatedTreatmentSquamous Cell Carcinoma (SCC)1
2Unknown StatusTreatmentLymphoma, Hodgkins1
2Unknown StatusTreatmentRecurrent or Refractory Primary CNS Lymphoma1
2Unknown StatusTreatmentRenal Cell Adenocarcinoma1
2Unknown StatusTreatmentUnresectable or Metastatic Hepatocellular Carcinoma1
2WithdrawnTreatmentMelanoma / Recurrent Melanoma / Stage III Melanoma / Stage IV Melanoma1
2WithdrawnTreatmentNeoplasms, Hepatic1
3Active Not RecruitingTreatmentPRETEXT Stage 1 Hepatoblastoma / PRETEXT Stage 2 Hepatoblastoma / PRETEXT Stage 3 Hepatoblastoma / PRETEXT Stage 4 Hepatoblastoma1
3CompletedTreatmentMalignant Lymphomas1
3CompletedTreatmentMantle Cell Lymphoma (MCL)1
3CompletedTreatmentNeoplasms, Kidney / Renal Cell Adenocarcinoma1
3CompletedTreatmentRenal Cell Adenocarcinoma2
3SuspendedTreatmentBotryoid-Type Embryonal Rhabdomyosarcoma / Rhabdomyosarcoma, Alveolar / Rhabdomyosarcoma, Embryonal / Rhabdomyosarcomas / Sclerosing Rhabdomyosarcoma / Spindle Cell Rhabdomyosarcoma / Untreated Childhood Rhabdomyosarcoma1
4CompletedTreatmentNon-Hodgkin's Lymphoma (NHL)1
4WithdrawnNot AvailableRenal Cell Adenocarcinoma1
Not AvailableCompletedNot AvailableRenal Cell Adenocarcinoma2
Not AvailableCompletedNot AvailableSquamous Cell Carcinoma (SCC)1
Not AvailableCompletedPreventionProstatic Neoplasms1
Not AvailableCompletedTreatmentRenal Cell Adenocarcinoma1
Not AvailableCompletedTreatmentTumors, Solid1
Not AvailableRecruitingNot AvailableCarcinoma, Renal Cell, Advanced / Gastrointestinal Stroma Tumors / Mantle Cell Lymphoma (MCL)1
Not AvailableRecruitingTreatmentRenal Cancers1
Not AvailableWithdrawnTreatmentHead and Neck Carcinoma1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Ben Venue Laboratories Inc.
  • Chunghwa Chemical Synthesis and Biotech Co. Ltd.
  • Pierre Fabre
  • Wyeth Pharmaceuticals
Dosage forms
FormRouteStrength
SolutionIntravenous25 mg
Injection, solution, concentrateIntravenous30 mg
Kit25 mg/1mL
LiquidIntravenous25 mg
Prices
Unit descriptionCostUnit
Torisel 25 mg kit1467.89USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2429020No2009-05-262021-11-13Canada
CA2187024No2004-08-102015-04-14Canada
US8791097Yes2012-11-102032-11-10Us
US8455539Yes2004-01-252024-01-25Us
US5362718Yes1999-08-152019-08-15Us
US8722700Yes2004-01-252024-01-25Us
US8026276Yes2006-07-202026-07-20Us
USRE44768Yes1999-08-152019-08-15Us
US8299116Yes2004-01-252024-01-25Us

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00235 mg/mLALOGPS
logP4.39ALOGPS
logP7.13ChemAxon
logS-5.6ALOGPS
pKa (Strongest Acidic)9.96ChemAxon
pKa (Strongest Basic)-2.9ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count14ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area241.96 Å2ChemAxon
Rotatable Bond Count11ChemAxon
Refractivity277.07 m3·mol-1ChemAxon
Polarizability112.71 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption-0.8908
Blood Brain Barrier-0.9494
Caco-2 permeable-0.664
P-glycoprotein substrateSubstrate0.8122
P-glycoprotein inhibitor IInhibitor0.8098
P-glycoprotein inhibitor IIInhibitor0.7467
Renal organic cation transporterNon-inhibitor0.7636
CYP450 2C9 substrateNon-substrate0.8699
CYP450 2D6 substrateNon-substrate0.8845
CYP450 3A4 substrateSubstrate0.7533
CYP450 1A2 substrateNon-inhibitor0.9126
CYP450 2C9 inhibitorNon-inhibitor0.8957
CYP450 2D6 inhibitorNon-inhibitor0.942
CYP450 2C19 inhibitorNon-inhibitor0.9155
CYP450 3A4 inhibitorNon-inhibitor0.9558
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9398
Ames testNon AMES toxic0.6087
CarcinogenicityNon-carcinogens0.9367
BiodegradationNot ready biodegradable0.9522
Rat acute toxicity2.8760 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9703
hERG inhibition (predictor II)Non-inhibitor0.7479
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as macrolide lactams. These are cyclic polyketides containing both a cyclic amide and a cyclic ester group.
Kingdom
Organic compounds
Super Class
Phenylpropanoids and polyketides
Class
Macrolide lactams
Sub Class
Not Available
Direct Parent
Macrolide lactams
Alternative Parents
Alpha amino acid esters / Macrolides and analogues / Beta hydroxy acids and derivatives / Piperidines / Oxanes / Dicarboxylic acids and derivatives / Tertiary carboxylic acid amides / Secondary alcohols / Carboxylic acid esters / Cyclic ketones
show 11 more
Substituents
Macrolide lactam / Alpha-amino acid ester / Macrolide / Alpha-amino acid or derivatives / Beta-hydroxy acid / Dicarboxylic acid or derivatives / Hydroxy acid / Oxane / Piperidine / Tertiary carboxylic acid amide
show 25 more
Molecular Framework
Aliphatic heteropolycyclic compounds
External Descriptors
lactam, macrolide (CHEBI:79699)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Tfiiic-class transcription factor binding
Specific Function
Serine/threonine protein kinase which is a central regulator of cellular metabolism, growth and survival in response to hormones, growth factors, nutrients, energy and stress signals. MTOR directly...
Gene Name
MTOR
Uniprot ID
P42345
Uniprot Name
Serine/threonine-protein kinase mTOR
Molecular Weight
288889.05 Da
References
  1. Patard JJ, Pouessel D, Bensalah K, Culine S: Targeted therapy in renal cell carcinoma. World J Urol. 2008 Apr;26(2):135-40. doi: 10.1007/s00345-008-0237-4. Epub 2008 Feb 12. [PubMed:18265991]
  2. Radulovic S, Bjelogrlic SK: Sunitinib, sorafenib and mTOR inhibitors in renal cancer. J BUON. 2007 Sep;12 Suppl 1:S151-62. [PubMed:17935273]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da

Drug created on March 19, 2008 10:22 / Updated on October 16, 2018 05:48