Stem definition | Drug id | CAS RN |
---|---|---|
immunosuppressants, rapamycin derivatives | 4161 | 162635-04-3 |
Dose | Unit | Route |
---|---|---|
3.57 | mg | P |
Property | Value | Reference |
---|---|---|
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
S (Water solubility) | 0.01 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
EoM (Fraction excreted unchanged in urine) | 4.60 % | Benet LZ, Broccatelli F, Oprea TI |
MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.15 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Vd (Volume of distribution) | 3 L/kg | Lombardo F, Berellini G, Obach RS |
CL (Clearance) | 7.70 mL/min/kg | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 18 hours | Lombardo F, Berellini G, Obach RS |
Date | Agency | Company | Orphan |
---|---|---|---|
Nov. 19, 2007 | EMA | Pfizer Limited | |
May 30, 2007 | FDA | PF PRISM CV |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Disease progression | 248.36 | 29.02 | 113 | 2484 | 95753 | 50506774 |
Hyperglycaemia | 58.11 | 29.02 | 31 | 2566 | 36374 | 50566153 |
Dehydration | 54.70 | 29.02 | 52 | 2545 | 152397 | 50450130 |
Death | 46.13 | 29.02 | 69 | 2528 | 325310 | 50277217 |
Hypophosphataemia | 42.28 | 29.02 | 16 | 2581 | 8398 | 50594129 |
Mucosal inflammation | 42.09 | 29.02 | 26 | 2571 | 40116 | 50562411 |
Hypokalaemia | 41.37 | 29.02 | 35 | 2562 | 87957 | 50514570 |
Stomatitis | 40.99 | 29.02 | 37 | 2560 | 101307 | 50501220 |
Hypertriglyceridaemia | 37.12 | 29.02 | 13 | 2584 | 5478 | 50597049 |
Pneumonitis | 35.81 | 29.02 | 21 | 2576 | 29489 | 50573038 |
Blood creatinine increased | 33.15 | 29.02 | 29 | 2568 | 76131 | 50526396 |
Febrile neutropenia | 30.63 | 29.02 | 31 | 2566 | 97636 | 50504891 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Disease progression | 500.72 | 24.01 | 264 | 5440 | 81652 | 29487171 |
Interstitial lung disease | 93.32 | 24.01 | 82 | 5622 | 57636 | 29511187 |
Neoplasm progression | 88.13 | 24.01 | 51 | 5653 | 18561 | 29550262 |
Stomatitis | 85.85 | 24.01 | 65 | 5639 | 37048 | 29531775 |
Pneumonitis | 85.25 | 24.01 | 58 | 5646 | 27986 | 29540837 |
Pleural effusion | 69.21 | 24.01 | 77 | 5627 | 71831 | 29496992 |
Dehydration | 50.51 | 24.01 | 84 | 5620 | 114664 | 29454159 |
Thrombocytopenia | 44.40 | 24.01 | 87 | 5617 | 134736 | 29434087 |
Mucosal inflammation | 43.36 | 24.01 | 41 | 5663 | 31554 | 29537269 |
Hypertriglyceridaemia | 42.19 | 24.01 | 23 | 5681 | 7452 | 29561371 |
Pneumocystis jirovecii pneumonia | 33.57 | 24.01 | 27 | 5677 | 16752 | 29552071 |
Drug ineffective | 32.20 | 24.01 | 15 | 5689 | 363155 | 29205668 |
Pneumonia | 31.25 | 24.01 | 133 | 5571 | 320039 | 29248784 |
Febrile neutropenia | 29.40 | 24.01 | 66 | 5638 | 112174 | 29456649 |
Renal cell carcinoma | 28.03 | 24.01 | 15 | 5689 | 4681 | 29564142 |
Lymphocyte count decreased | 26.41 | 24.01 | 25 | 5679 | 19246 | 29549577 |
Blood triglycerides increased | 26.41 | 24.01 | 21 | 5683 | 12813 | 29556010 |
Osteonecrosis of jaw | 25.70 | 24.01 | 23 | 5681 | 16487 | 29552336 |
Extravasation | 24.67 | 24.01 | 10 | 5694 | 1662 | 29567161 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Disease progression | 554.70 | 25.30 | 265 | 5600 | 141415 | 64351452 |
Stomatitis | 125.26 | 25.30 | 93 | 5772 | 109512 | 64383355 |
Neoplasm progression | 94.33 | 25.30 | 54 | 5811 | 40910 | 64451957 |
Dehydration | 90.98 | 25.30 | 105 | 5760 | 216658 | 64276209 |
Febrile neutropenia | 77.18 | 25.30 | 90 | 5775 | 187567 | 64305300 |
Interstitial lung disease | 69.53 | 25.30 | 63 | 5802 | 97669 | 64395198 |
Pneumonitis | 69.52 | 25.30 | 48 | 5817 | 50317 | 64442550 |
Pleural effusion | 61.04 | 25.30 | 66 | 5799 | 126493 | 64366374 |
Hyperglycaemia | 59.15 | 25.30 | 47 | 5818 | 60921 | 64431946 |
Hypertriglyceridaemia | 52.89 | 25.30 | 24 | 5841 | 11181 | 64481686 |
Thrombocytopenia | 48.80 | 25.30 | 79 | 5786 | 223722 | 64269145 |
Mucosal inflammation | 47.75 | 25.30 | 42 | 5823 | 62542 | 64430325 |
Pneumocystis jirovecii pneumonia | 42.07 | 25.30 | 28 | 5837 | 27606 | 64465261 |
Renal cell carcinoma | 41.75 | 25.30 | 17 | 5848 | 6087 | 64486780 |
Pneumonia | 41.48 | 25.30 | 128 | 5737 | 559448 | 63933419 |
Death | 41.07 | 25.30 | 116 | 5749 | 482589 | 64010278 |
Blood bilirubin increased | 38.74 | 25.30 | 36 | 5829 | 57517 | 64435350 |
Lymphocyte count decreased | 38.65 | 25.30 | 31 | 5834 | 40668 | 64452199 |
Hypophosphataemia | 35.45 | 25.30 | 20 | 5845 | 14700 | 64478167 |
Blood creatinine increased | 33.81 | 25.30 | 51 | 5814 | 135731 | 64357136 |
Hypokalaemia | 32.09 | 25.30 | 47 | 5818 | 121856 | 64371011 |
Proteinuria | 30.41 | 25.30 | 23 | 5842 | 27700 | 64465167 |
Drug ineffective | 29.87 | 25.30 | 20 | 5845 | 840227 | 63652640 |
Anaemia | 29.25 | 25.30 | 88 | 5777 | 378592 | 64114275 |
Neutrophil count decreased | 28.32 | 25.30 | 35 | 5830 | 77161 | 64415706 |
Blood triglycerides increased | 26.05 | 25.30 | 18 | 5847 | 18848 | 64474019 |
Platelet count decreased | 25.93 | 25.30 | 51 | 5814 | 167660 | 64325207 |
Metastatic renal cell carcinoma | 25.48 | 25.30 | 9 | 5856 | 2187 | 64490680 |
None
Source | Code | Description |
---|---|---|
ATC | L01EG01 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Mammalian target of rapamycin (mTOR) kinase inhibitors |
FDA MoA | N0000175076 | Protein Kinase Inhibitors |
FDA PE | N0000175550 | Decreased Immunologic Activity |
MeSH PA | D000970 | Antineoplastic Agents |
MeSH PA | D004791 | Enzyme Inhibitors |
MeSH PA | D007155 | Immunologic Factors |
MeSH PA | D007166 | Immunosuppressive Agents |
MeSH PA | D000091203 | MTOR Inhibitors |
MeSH PA | D047428 | Protein Kinase Inhibitors |
CHEBI has role | CHEBI:35610 | antineoplastic agents |
CHEBI has role | CHEBI:35705 | immunosuppressive agents |
CHEBI has role | CHEBI:36047 | antibacterial drugs |
CHEBI has role | CHEBI:68481 | mTOR inhibitors |
CHEBI has role | CHEBI:149553 | anticoronaviral drug |
CHEBI has role | CHEBI:176497 | geroprotectors |
FDA EPC | N0000175605 | Kinase Inhibitor |
FDA MoA | N0000175624 | mTOR Inhibitors |
FDA EPC | N0000175625 | mTOR Inhibitor Immunosuppressant |
MeSH PA | D000900 | Anti-Bacterial Agents |
MeSH PA | D000890 | Anti-Infective Agents |
MeSH PA | D000903 | Antibiotics, Antineoplastic |
MeSH PA | D000935 | Antifungal Agents |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Mantle cell lymphoma | indication | 443487006 | |
Renal cell carcinoma | indication | 702391001 | DOID:4450 |
Hyperbilirubinemia | contraindication | 14783006 | DOID:2741 |
Gastrointestinal perforation | contraindication | 51875005 | |
Hyperlipidemia | contraindication | 55822004 | DOID:1168 |
Acute infectious disease | contraindication | 63171007 | |
Interstitial pneumonia | contraindication | 64667001 | |
Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
Hyperglycemia | contraindication | 80394007 | DOID:4195 |
Kidney disease | contraindication | 90708001 | DOID:557 |
Secondary malignant neoplasm of cerebrum | contraindication | 94248000 | |
Perioperative care | contraindication | 133897009 | |
Cerebrovascular accident | contraindication | 230690007 | |
Disease of liver | contraindication | 235856003 | DOID:409 |
Impaired wound healing | contraindication | 271618001 | |
Pregnancy, function | contraindication | 289908002 | |
Surgical procedure | contraindication | 387713003 | |
Breastfeeding (mother) | contraindication | 413712001 | |
Malignant neoplasm of brain | contraindication | 428061005 | DOID:1319 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 10.5 | acidic |
pKa2 | 13.82 | acidic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
---|---|---|---|---|---|---|---|---|---|---|
25MG/ML (25MG/ML) | TORISEL | PF PRISM CV | N022088 | May 30, 2007 | RX | SOLUTION | INTRAVENOUS | 8791097 | May 10, 2032 | METHOD OF TREATING METASTATIC PAPILLARY RENAL CELL CARCINOMA WITH TEMSIROLIMUS. |
25MG/ML (25MG/ML) | TORISEL | PF PRISM CV | N022088 | May 30, 2007 | RX | SOLUTION | INTRAVENOUS | 8791097 | May 10, 2032 | METHOD OF TREATING PAPILLARY RENAL CELL CARCINOMA WITH TEMSIROLIMUS, IN THE ABSENCE OF INTERFERON ALPHA. |
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Peptidyl-prolyl cis-trans isomerase FKBP1A | Enzyme | INHIBITOR | CHEMBL | CHEMBL | |||||
Multidrug resistance protein 1 | Transporter | WOMBAT-PK | |||||||
Serine/threonine-protein kinase mTOR | Kinase | IC50 | 5.75 | CHEMBL | |||||
Peptidyl-prolyl cis-trans isomerase FKBP3 | Enzyme | WOMBAT-PK |
ID | Source |
---|---|
4026239 | VUID |
N0000179796 | NUI |
D06068 | KEGG_DRUG |
4021176 | VANDF |
4026239 | VANDF |
C1707080 | UMLSCUI |
CHEBI:79699 | CHEBI |
CHEBI:9168 | CHEBI |
A4I | PDB_CHEM_ID |
CHEMBL1201182 | ChEMBL_ID |
DB06287 | DRUGBANK_ID |
C401859 | MESH_SUPPLEMENTAL_RECORD_UI |
5892 | IUPHAR_LIGAND_ID |
8212 | INN_ID |
624KN6GM2T | UNII |
6918289 | PUBCHEM_CID |
DB00877 | DRUGBANK_ID |
35302 | RXNORM |
110527 | MMSL |
210889 | MMSL |
23908 | MMSL |
287829 | MMSL |
8303 | MMSL |
d04453 | MMSL |
d06836 | MMSL |
007885 | NDDF |
012233 | NDDF |
116109004 | SNOMEDCT_US |
387014003 | SNOMEDCT_US |
427153004 | SNOMEDCT_US |
427299005 | SNOMEDCT_US |
5284616 | PUBCHEM_CID |
C0072980 | UMLSCUI |
D020123 | MESH_DESCRIPTOR_UI |
7104 | INN_ID |
None