TEGAFUR

First approved in 1962

Details

Stereochemistry	RACEMIC
Molecular Formula	C8H9FN2O3
Molecular Weight	200.1671
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

FC1=CN(C2CCCO2)C(=O)NC1=O

InChI

InChIKey=WFWLQNSHRPWKFK-UHFFFAOYSA-N

InChI=1S/C8H9FN2O3/c9-5-4-11(6-2-1-3-14-6)8(13)10-7(5)12/h4,6H,1-3H2,(H,10,12,13)

HIDE SMILES / InChI

Molecular Formula	C8H9FN2O3
Molecular Weight	200.1671
Charge	0
Count

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description
Sources: http://home.intekom.com/pharm/bm_squib/uft.htmlhttp://www.drugbank.ca/drugs/DB00544
Curator's Comment: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/012209s040lbl.pdf

Fluorouracil is an antineoplastic anti-metabolite. Anti-metabolites masquerade as purine or pyrimidine - which become the building blocks of DNA. They prevent these substances from becoming incorporated into DNA during the "S" phase (of the cell cycle), stopping normal development and division. Fluorouracil blocks an enzyme which converts the cytosine nucleotide into the deoxy derivative. In addition, DNA synthesis is further inhibited because Fluorouracil blocks the incorporation of the thymidine nucleotide into the DNA strand. Fluorouracil is used for the topical treatment of multiple actinic or solar keratoses. In the 5% strength it is also useful in the treatment of superficial basal cell carcinomas when conventional methods are impractical, such as with multiple lesions or difficult treatment sites. Fluorouracil injection is indicated in the palliative management of some types of cancer, including colon, esophageal, gastric, rectum, breast, biliary tract, stomach, head and neck, cervical, pancreas, renal cell, and carcinoid.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Thymidylate synthase 32 Target ID: CHEMBL1952 Sources: http://www.drugbank.ca/drugs/DB00544	Inhibitor 8297
Thymidylate synthase 32 Target ID: CHEMBL1952 Sources: http://home.intekom.com/pharm/bm_squib/uft.html	Inhibitor 8297
Colon carcinoma cells 4 Target ID: CHEMBL614464 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27503679	Inhibitor 8297	29.5 µM [IC50]
PC-3 15 Target ID: CHEMBL390 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19423198	Inhibitor 8297	16.0 nM [IC50]
AGS 4 Target ID: CHEMBL613860 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26821004	Inhibitor 8297	43.8 µM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
Head and neck cancer 50 Sources: http://www.229877.com/article/2013/1127/article_33601.html	Primary	Approved 8429	UFT E combination granule T100 / T150 Approved Use in the treatment of head and neck cancer, gastric cancer, colorectal cancer, hepatic cancer, gallbladder cancer, bile-duct cancer, pancreatic cancer, lung cancer, breast cancer, bladder cancer, prostatic cancer, or uterine cervical cancer.
Digestive system neoplasms 4 Sources: http://www.229877.com/article/2013/1127/article_33601.html	Primary	Approved 8429	UFT E combination granule T100 / T150 Approved Use in the treatment of head and neck cancer, gastric cancer, colorectal cancer, hepatic cancer, gallbladder cancer, bile-duct cancer, pancreatic cancer, lung cancer, breast cancer, bladder cancer, prostatic cancer, or uterine cervical cancer.
Prostate cancer 178 Sources: http://www.229877.com/article/2013/1127/article_33601.html	Primary	Approved 8429	UFT E combination granule T100 / T150 Approved Use in the treatment of head and neck cancer, gastric cancer, colorectal cancer, hepatic cancer, gallbladder cancer, bile-duct cancer, pancreatic cancer, lung cancer, breast cancer, bladder cancer, prostatic cancer, or uterine cervical cancer.
Lung cancer 69 Sources: http://www.229877.com/article/2013/1127/article_33601.html	Primary	Approved 8429	UFT E combination granule T100 / T150 Approved Use in the treatment of head and neck cancer, gastric cancer, colorectal cancer, hepatic cancer, gallbladder cancer, bile-duct cancer, pancreatic cancer, lung cancer, breast cancer, bladder cancer, prostatic cancer, or uterine cervical cancer.
Breast cancer 434 Sources: http://www.229877.com/article/2013/1127/article_33601.html	Primary	Approved 8429	UFT E combination granule T100 / T150 Approved Use in the treatment of head and neck cancer, gastric cancer, colorectal cancer, hepatic cancer, gallbladder cancer, bile-duct cancer, pancreatic cancer, lung cancer, breast cancer, bladder cancer, prostatic cancer, or uterine cervical cancer.
Adenocarcinoma of the colon 4 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/012209s040lbl.pdf	Primary	Approved 8429	FLUOROURACIL Approved Use Fluorouracil is indicated for the treatment of patients with: Adenocarcinoma of the Colon and Rectum Adenocarcinoma of the Breast Gastric Adenocarcinoma Pancreatic Adenocarcinoma Launch Date 1962
Gastric adenocarcinoma 12 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/012209s040lbl.pdf	Primary	Approved 8429	FLUOROURACIL Approved Use Fluorouracil is indicated for the treatment of patients with: Adenocarcinoma of the Colon and Rectum Adenocarcinoma of the Breast Gastric Adenocarcinoma Pancreatic Adenocarcinoma Launch Date 1962
Breast adenocarcinoma 7 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/012209s040lbl.pdf	Primary	Approved 8429	FLUOROURACIL Approved Use Fluorouracil is indicated for the treatment of patients with: Adenocarcinoma of the Colon and Rectum Adenocarcinoma of the Breast Gastric Adenocarcinoma Pancreatic Adenocarcinoma Launch Date 1962

C_max

Value	Dose	Co-administered	Analyte	Population
11.49 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/20985lbl.pdf	1 g 2 times / day steady-state, topical dose: 1 g route of administration: Topical experiment type: STEADY-STATE co-administered:		FLUOROURACIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
278 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/12907286	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:		FLUOROURACIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2046.2 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/31011915	80 mg 2 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered: GIMERACIL	GIMERACIL	TEGAFUR plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
22.39 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/20985lbl.pdf	1 g 2 times / day steady-state, topical dose: 1 g route of administration: Topical experiment type: STEADY-STATE co-administered:		FLUOROURACIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
205 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/12907286	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:		FLUOROURACIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
10786 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/31011915	80 mg 2 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered: GIMERACIL	GIMERACIL	TEGAFUR plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
0.24 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/12907286	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:		FLUOROURACIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
8.5 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/31011915	80 mg 2 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered: GIMERACIL	GIMERACIL	TEGAFUR plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
90% EXPERIMENT http://www.acutetox.eu/pdf_human_short/17-5-fluorouracil%20revised.pdf			FLUOROURACIL plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN
47.7% OTHER GOV https://www.ema.europa.eu/en/documents/product-information/teysuno-epar-product-information_en.pdf			TEGAFUR serum	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
3400 mg/m2 1 times / week multiple, intravenous Highest studied dose Dose: 3400 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 3400 mg/m2, 1 times / week Sources: https://pubmed.ncbi.nlm.nih.gov/3373260	unhealthy, 54 years (range: 24-78 years) n = 8 Health Status: unhealthy Condition: Advanced Pancreatic Cancer\| Colorectal Cancer Age Group: 54 years (range: 24-78 years) Sex: M+F Population Size: 8 Sources: https://pubmed.ncbi.nlm.nih.gov/3373260	DLT: Ataxia... Other AEs: Anorexia, Nausea... Dose limiting toxicities: Ataxia (grade 3, 4 patients) Other AEs: Anorexia (3 patients) Nausea (severe, 2 patients) Vomiting (2 patients) Stomatitis (severe, 1 patient) Diarrhea (3 patients) Weakness (1 patient) Hair loss (1 patient) Peeling (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/3373260
2600 mg/m2 1 times / week multiple, intravenous MTD Dose: 2600 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 2600 mg/m2, 1 times / week Sources: https://pubmed.ncbi.nlm.nih.gov/3373260	unhealthy, 54 years (range: 24-78 years) n = 8 Health Status: unhealthy Condition: Advanced Pancreatic Cancer\| Colorectal Cancer Age Group: 54 years (range: 24-78 years) Sex: M+F Population Size: 8 Sources: https://pubmed.ncbi.nlm.nih.gov/3373260	Other AEs: Ataxia, Anorexia... Other AEs: Ataxia (3 patients) Anorexia (4 patients) Nausea (severe, 2 patients) Vomiting (3 patients) Stomatitis (mild, 3 patients) Diarrhea (2 patients) Weakness (2 patients) Hair loss (2 patients) Loss of eyelashes (1 patient) Peeling (2 patients) Peeling (2 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/3373260
2800 mg/m2 1 times / week multiple, intravenous Dose: 2800 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 2800 mg/m2, 1 times / week Sources: https://pubmed.ncbi.nlm.nih.gov/8262730	unhealthy, 59 years n = 3 Health Status: unhealthy Age Group: 59 years Sex: M+F Population Size: 3 Sources: https://pubmed.ncbi.nlm.nih.gov/8262730	DLT: Diarrhea... Dose limiting toxicities: Diarrhea (grade 3, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/8262730
3000 mg/m2 1 times / week multiple, intravenous Dose: 3000 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 3000 mg/m2, 1 times / week Sources: https://pubmed.ncbi.nlm.nih.gov/8262730	unhealthy, 59 years n = 14 Health Status: unhealthy Age Group: 59 years Sex: M+F Population Size: 14 Sources: https://pubmed.ncbi.nlm.nih.gov/8262730	DLT: Diarrhea... Dose limiting toxicities: Diarrhea (grade 3-4, 2 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/8262730
3250 mg/m2 1 times / week multiple, intravenous Dose: 3250 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 3250 mg/m2, 1 times / week Sources: https://pubmed.ncbi.nlm.nih.gov/8262730	unhealthy, 59 years n = 9 Health Status: unhealthy Age Group: 59 years Sex: M+F Population Size: 9 Sources: https://pubmed.ncbi.nlm.nih.gov/8262730	DLT: Diarrhea... Dose limiting toxicities: Diarrhea (grade 3-4, 2 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/8262730
0.5 % 1 times / day multiple, topical Recommended Dose: 0.5 %, 1 times / day Route: topical Route: multiple Dose: 0.5 %, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/20985lbl.pdf	unhealthy, adult n = 257 Health Status: unhealthy Condition: actinic keratoses Age Group: adult Sex: M+F Population Size: 257 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/20985lbl.pdf	Disc. AE: Irritation skin... AEs leading to discontinuation/dose reduction: Irritation skin (12%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/20985lbl.pdf
1250 mg 1 times / 2 days multiple, oral Dose: 1250 mg, 1 times / 2 days Route: oral Route: multiple Dose: 1250 mg, 1 times / 2 days Sources: https://pubmed.ncbi.nlm.nih.gov/7302355	unhealthy, adult n = 7 Health Status: unhealthy Condition: hepatoma Age Group: adult Population Size: 7 Sources: https://pubmed.ncbi.nlm.nih.gov/7302355	Sources: https://pubmed.ncbi.nlm.nih.gov/7302355
500 mg single, oral Dose: 500 mg Route: oral Route: single Dose: 500 mg Sources: https://pubmed.ncbi.nlm.nih.gov/7463330	unhealthy, adult n = 6 Health Status: unhealthy Condition: breast cancer Age Group: adult Sex: F Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/7463330	Sources: https://pubmed.ncbi.nlm.nih.gov/7463330
5 % 2 times / day steady, topical Dose: 5 %, 2 times / day Route: topical Route: steady Dose: 5 %, 2 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT00847912	unhealthy n = 468 Health Status: unhealthy Condition: Keratinocyte carcinoma Population Size: 468 Sources: https://clinicaltrials.gov/ct2/show/NCT00847912	Other AEs: Anaemia, Angina unstable... Other AEs: Anaemia (serious, 2 patients) Angina unstable (serious, 5 patients) Arrhythmia (serious, 2 patients) Arteriosclerosis coronary artery (serious, 1 patient) Atrial flutter (serious, 3 patients) Atrial tachycardia (serious, 1 patient) Atrial thrombosis (serious, 1 patient) Cardiac disorder (serious, 1 patient) Cardiac failure congestive (serious, 7 patients) Cardio-respiratory arrest (serious, 2 patients) Coronary artery stenosis (serious, 1 patient) Myocardial ischaemia (serious, 1 patient) Palpitations (serious, 1 patient) Pericarditis (serious, 1 patient) Ventricular tachycardia (serious, 2 patients) Vertigo (serious, 1 patient) Vertigo positional (serious, 1 patient) Disorder vestibular (serious, 1 patient) Goitre (serious, 1 patient) Inappropriate antidiuretic hormone secretion (serious, 1 patient) Abdominal hernia (serious, 1 patient) Colitis ischaemic (serious, 1 patient) Gastritis (serious, 2 patients) Haemorrhoids (serious, 1 patient) Impaired gastric emptying (serious, 1 patient) Hernia inguinal (serious, 1 patient) Intestinal obstruction (serious, 2 patients) Obstruction gastric (serious, 1 patient) Oesophageal obstruction (serious, 1 patient) Pancreatitis (serious, 1 patient) Vomiting (serious, 1 patient) Adhesion (serious, 1 patient) Chest discomfort (serious, 1 patient) Generalised oedema (serious, 1 patient) Non-cardiac chest pain (serious, 3 patients) Cholelithiasis (serious, 2 patients) Hepatitis alcoholic (serious, 1 patient) Arthritis infective (serious, 1 patient) Bacteraemia (serious, 1 patient) Bronchopneumonia (serious, 1 patient) Cholecystitis infective (serious, 1 patient) Clostridium difficile infection (serious, 3 patients) Cystitis (serious, 1 patient) Endocarditis (serious, 1 patient) Incision site cellulitis (serious, 1 patient) Infection (serious, 2 patients) Septic shock (serious, 1 patient) Upper respiratory tract infection (serious, 1 patient) Urinary tract infection (serious, 6 patients) Viral infection (serious, 1 patient) Device toxicity (serious, 1 patient) Fall (serious, 11 patient) Hip fracture (serious, 2 patients) Intentional overdose (serious, 1 patient) Limb injury (serious, 1 patient) Lower limb fracture (serious, 1 patient) Meniscus injury (serious, 2 patients) Periprosthetic fracture (serious, 1 patient) Postoperative fever (serious, 1 patient) Procedural nausea (serious, 1 patient) Procedural pain (serious, 1 patient) Radiation oesophagitis (serious, 1 patient) Road traffic accident (serious, 2 patients) Traumatic haematoma (serious, 1 patient) Vascular bypass dysfunction (serious, 1 patient) Blood glucose increased (serious, 1 patient) Electrocardiogram abnormal (serious, 1 patient) Haemoglobin decreased (serious, 1 patient) International normalised ratio increased (serious, 2 patients) White blood cell count increased (serious, 1 patient) Dehydration (serious, 5 patients) Diabetes mellitus inadequate control (serious, 2 patients) Failure to thrive (serious, 3 patients) Hyperglycaemia (serious, 2 patients) Hyponatraemia (serious, 3 patients) Iron deficiency (serious, 1 patient) Arthralgia (serious, 3 patients) Bursa disorder (serious, 1 patient) Exostosis (serious, 1 patient) Muscular weakness (serious, 1 patient) Osteoarthritis (serious, 10 patients) Tendonitis (serious, 1 patient) Basal cell carcinoma (serious, 1 patient) Benign salivary gland neoplasm (serious, 1 patient) Brain neoplasm (serious, 2 patients) Colorectal cancer (serious, 1 patient) Diffuse large B-cell lymphoma stage IV (serious, 1 patient) Haemangioma (serious, 1 patient) Lung neoplasm malignant (serious, 4 patients) Malignant melanoma (serious, 3 patients) Metastases to central nervous system (serious, 1 patient) Metastatic squamous cell carcinoma (serious, 1 patient) Neuroendocrine carcinoma (serious, 1 patient) Prostate cancer (serious, 5 patients) Prostate cancer recurrent (serious, 1 patient) Renal cancer (serious, 2 patients) Renal cancer metastatic (serious, 1 patient) Renal cell carcinoma (serious, 1 patient) Salivary gland cancer (serious, 1 patient) Squamous cell carcinoma (serious, 2 patients) Basilar artery stenosis (serious, 1 patient) Cognitive disorder (serious, 1 patient) Dementia (serious, 4 patients) Epilepsy (serious, 1 patient) Headache (serious, 1 patient) Hypoaesthesia (serious, 1 patient) Parkinson's disease (serious, 2 patients) Haemorrhage subarachnoid (serious, 1 patient) Transient ischaemic attack (serious, 4 patients) Transient ischaemic attack (serious, 4 patients) Dementia vascular (serious, 1 patient) Alcohol abuse (serious, 2 patients) Binge drinking (serious, 1 patient) Completed suicide (serious, 1 patient) Confusional state (serious, 1 patient) Delirium tremens (serious, 1 patient) Depression (serious, 3 patients) Mental disorder (serious, 1 patient) Mental status changes (serious, 2 patients) Post-traumatic stress disorder (serious, 1 patient) Suicidal behaviour (serious, 1 patient) Suicidal ideation (serious, 3 patients) Hydronephrosis (serious, 2 patients) Nephropathy (serious, 1 patient) Renal failure chronic (serious, 1 patient) Erectile dysfunction (serious, 1 patient) Prostatic haemorrhage (serious, 1 patient) Prostatitis (serious, 1 patient) Chronic obstructive pulmonary disease (serious, 9 patients) Dyspnoea (serious, 2 patients) Dyspnoea exertional (serious, 1 patient) Haemoptysis (serious, 1 patient) Pleural effusion (serious, 1 patient) Pulmonary embolism (serious, 3 patients) Respiratory failure (serious, 1 patient) Rash (serious, 1 patient) Angioplasty (serious, 1 patient) Cholecystectomy (serious, 1 patient) Coronary angioplasty (serious, 1 patient) Elective procedure (serious, 1 patient) Hip arthroplasty (serious, 1 patient) Knee arthroplasty (serious, 1 patient) Medical device removal (serious, 1 patient) Oesophagogastric fundoplasty (serious, 1 patient) Parotidectomy (serious, 1 patient) Wound treatment (serious, 1 patient) Aortic aneurysm (serious, 2 patients) Aortic occlusion (serious, 1 patient) Arterial occlusive disease (serious, 1 patient) Femoral artery occlusion (serious, 1 patient) Labile hypertension (serious, 1 patient) Orthostatic hypotension (serious, 2 patients) Disorder peripheral vascular (serious, 1 patient) Lymphadenopathy (below serious, 1 patient) Vertigo (below serious, 1 patient) Adrenal mass (below serious, 1 patient) Eye haemorrhage (below serious, 1 patient) Eye irritation (below serious, 3 patients) Eye pain (below serious, 2 patients) Eye pruritus (below serious, 1 patient) Eye swelling (below serious, 4 patients) Photophobia (below serious, 1 patient) Visual acuity reduced (below serious, 1 patient) Abdominal pain upper (below serious, 2 patients) Cheilitis (below serious, 1 patient) Diarrhoea (below serious, 3 patients) Diverticulum (below serious, 1 patient) Dyspepsia (below serious, 1 patient) Gastrooesophageal reflux disease (below serious, 1 patient) Gingival pain (below serious, 1 patient) Nausea (below serious, 5 patients) Fatigue (below serious, 3 patients) Feeling of body temperature change (below serious, 1 patient) Hernia (below serious, 1 patient) Local swelling (below serious, 1 patient) Malaise (below serious, 1 patient) Pain (below serious, 11 patient) Syringe issue (below serious, 1 patient) Temperature intolerance (below serious, 1 patient) Tenderness (below serious, 2 patients) Vessel puncture site haematoma (below serious, 1 patient) Hypersensitivity (below serious, 1 patient) Seasonal allergy (below serious, 1 patient) Bronchitis (below serious, 4 patients) Cellulitis (below serious, 1 patient) Folliculitis (below serious, 1 patient) Fungal infection (below serious, 1 patient) Herpes zoster (below serious, 2 patients) Infection (below serious, 2 patients) Influenza (below serious, 1 patient) Nasopharyngitis (below serious, 5 patients) Oral herpes (below serious, 1 patient) Pneumonia (below serious, 2 patients) Accidental exposure to product (below serious, 1 patient) Arthropod sting (below serious, 1 patient) Fall (below serious, 5 patients) Laceration (below serious, 1 patient) Muscle rupture (below serious, 1 patient) Body temperature increased (below serious, 1 patient) Emergency care examination (below serious, 1 patient) Gout (below serious, 1 patient) Arthralgia (below serious, 1 patient) Back pain (below serious, 3 patients) Foot deformity (below serious, 1 patient) Musculoskeletal pain (below serious, 1 patient) Neck pain (below serious, 1 patient) Pain in extremity (below serious, 1 patient) Polymyalgia rheumatica (below serious, 1 patient) Basal cell carcinoma (below serious, 1 patient) Haemangioma (below serious, 1 patient) Transitional cell carcinoma (below serious, 1 patient) Burning sensation (below serious, 1 patient) Dizziness (below serious, 4 patients) Headache (below serious, 5 patients) Hypoaesthesia (below serious, 2 patients) Syncope (below serious, 1 patient) Tunnel vision (below serious, 1 patient) Abnormal dreams (below serious, 1 patient) Anxiety (below serious, 1 patient) Psychotic disorder (below serious, 1 patient) Sleep disorder (below serious, 22 patients) Dysuria (below serious, 1 patient) Haemorrhage urinary tract (below serious, 1 patient) Pollakiuria (below serious, 1 patient) Chronic obstructive pulmonary disease (below serious, 1 patient) Nasal congestion (below serious, 1 patient) Productive cough (below serious, 1 patient) Pulmonary mass (below serious, 1 patient) Rhinorrhoea (below serious, 1 patient) Sinus disorder (below serious, 1 patient) Acne (below serious, 5 patients) Blister (below serious, 2 patients) Blood blister (below serious, 1 patient) Decubitus ulcer (below serious, 1 patient) Dermatitis (below serious, 447 patients) Dermatitis allergic (below serious, 1 patient) Hyperhidrosis (below serious, 2 patients) Photosensitivity reaction (below serious, 5 patients) Post inflammatory pigmentation change (below serious, 1 patient) Scab (below serious, 1 patient) Seborrhoea (below serious, 1 patient) Dermatitis seborrhoeic (below serious, 2 patients) Skin discomfort (below serious, 1 patient) Skin haemorrhage (below serious, 3 patients) Skin tightness (below serious, 1 patient) Skin ulcer (below serious, 1 patient) Urticaria (below serious, 1 patient) Oral surgery (below serious, 1 patient) Wound drainage (below serious, 1 patient) Haemorrhage (below serious, 7 patients) Temporal arteritis (below serious, 1 patient) Sources: https://clinicaltrials.gov/ct2/show/NCT00847912
111.6 mg/m2 1 times / day steady, oral RP2D Dose: 111.6 mg/m2, 1 times / day Route: oral Route: steady Dose: 111.6 mg/m2, 1 times / day Co-administed with:: uracil(248.4 mg/m2) Sources: https://pubmed.ncbi.nlm.nih.gov/9348565 https://pubmed.ncbi.nlm.nih.gov/8949982	unhealthy, 54 years n = 6 Health Status: unhealthy Condition: carcinoma Age Group: 54 years Sex: M+F Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/9348565 https://pubmed.ncbi.nlm.nih.gov/8949982	Other AEs: Fatigue, Nausea... Other AEs: Fatigue (grade 1-2, 3 patients) Nausea (grade 1-2, 2 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/9348565 https://pubmed.ncbi.nlm.nih.gov/8949982
248 mg/m2 1 times / day steady, oral RP2D Dose: 248 mg/m2, 1 times / day Route: oral Route: steady Dose: 248 mg/m2, 1 times / day Co-administed with:: uracil(552 mg/m2) Sources: https://pubmed.ncbi.nlm.nih.gov/9348565 https://pubmed.ncbi.nlm.nih.gov/8949982	unhealthy, 59 years n = 8 Health Status: unhealthy Condition: carcinoma Age Group: 59 years Sex: M+F Population Size: 8 Sources: https://pubmed.ncbi.nlm.nih.gov/9348565 https://pubmed.ncbi.nlm.nih.gov/8949982	Other AEs: Granulocytopenia, Nausea... Other AEs: Granulocytopenia (grade 4, 1 patient) Nausea (grade 3, 1 patient) Thrombocytopenia (grade 3, 1 patient) Vomiting (grade 1-2, 5 patients) Fatigue (grade 1-2, 4 patients) Diarrhoea (grade 1-2, 4 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/9348565 https://pubmed.ncbi.nlm.nih.gov/8949982
139.5 mg/m2 1 times / day steady, oral Highest studied dose Dose: 139.5 mg/m2, 1 times / day Route: oral Route: steady Dose: 139.5 mg/m2, 1 times / day Co-administed with:: uracil(310.5 mg/m2) Sources: https://pubmed.ncbi.nlm.nih.gov/9348565	unhealthy n = 6 Health Status: unhealthy Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/9348565	DLT: Diarrhea... Dose limiting toxicities: Diarrhea (grade 3-4, 3 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/9348565
279 mg/m2 1 times / day steady, oral Highest studied dose Dose: 279 mg/m2, 1 times / day Route: oral Route: steady Dose: 279 mg/m2, 1 times / day Co-administed with:: uracil(621 mg/m2) Sources: https://pubmed.ncbi.nlm.nih.gov/9348565	unhealthy n = 5 Health Status: unhealthy Population Size: 5 Sources: https://pubmed.ncbi.nlm.nih.gov/9348565	DLT: Granulocytopenia... Dose limiting toxicities: Granulocytopenia (grade 4, 4 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/9348565
124 mg/m2 1 times / day steady, oral Dose: 124 mg/m2, 1 times / day Route: oral Route: steady Dose: 124 mg/m2, 1 times / day Co-administed with:: uracil(276 mg/m2) Sources: https://pubmed.ncbi.nlm.nih.gov/9348565	unhealthy n = 8 Health Status: unhealthy Population Size: 8 Sources: https://pubmed.ncbi.nlm.nih.gov/9348565	DLT: Diarrhea... Dose limiting toxicities: Diarrhea (grade 3-4, 3 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/9348565

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1737 inhibitor 1587	substrate 1037 inhibitor 1767 supressor 19	substrate 1217 inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2A6 707 CYP1A1 110 CYP1A2 1524 CYP2C8 911 CYP2C19 1478 CYP2E1 882	CYP2A6 543 CYP1A1 349 CYP1A2 1054 CYP2B6 664 CYP2C8 693 CYP2C19 991 CYP2E1 667	CYP2B6 547 CYP2C8 168 CYP3A4/5 124

Drug as perpetrator

Target	Modality	Activity
CYP2A6 739	inhibitor 3277 Sources: https://www.ema.europa.eu/en/documents/assessment-report/teysuno-epar-public-assessment-report_en.pdf#page=18 Page: 18.0	no [IC50 3110 uM]
CYP1A1 218	inhibitor 3277 Sources: https://www.ema.europa.eu/en/documents/assessment-report/teysuno-epar-public-assessment-report_en.pdf#page=18 Page: 18.0	no
CYP1A2 1692	inhibitor 3277 Sources: https://jpet.aspetjournals.org/content/297/3/1166 Page: -	no
CYP1A2 1692	inhibitor 3277 Sources: https://www.ema.europa.eu/en/documents/assessment-report/teysuno-epar-public-assessment-report_en.pdf#page=18 Page: 18.0	no
CYP2C19 1553	inhibitor 3277 Sources: https://jpet.aspetjournals.org/content/297/3/1166 Page: -	no
CYP2C19 1553	inhibitor 3277 Sources: https://www.ema.europa.eu/en/documents/assessment-report/teysuno-epar-public-assessment-report_en.pdf#page=18 Page: 18.0	no
CYP2C8 965	inhibitor 3277 Sources: https://jpet.aspetjournals.org/content/297/3/1166 Page: -	no
CYP2C8 965	inhibitor 3277 Sources: https://www.ema.europa.eu/en/documents/assessment-report/teysuno-epar-public-assessment-report_en.pdf#page=18 Page: 18.0	no
CYP2C9 1819	inhibitor 3277 Sources: https://jpet.aspetjournals.org/content/297/3/1166 Page: -	no
CYP2C9 1819	inhibitor 3277 Sources: https://www.ema.europa.eu/en/documents/assessment-report/teysuno-epar-public-assessment-report_en.pdf#page=18 Page: 18.0	no
CYP2D6 1891	inhibitor 3277 Sources: https://jpet.aspetjournals.org/content/297/3/1166 Page: -	no
CYP2D6 1891	inhibitor 3277 Sources: https://www.ema.europa.eu/en/documents/assessment-report/teysuno-epar-public-assessment-report_en.pdf#page=18 Page: 18.0	no
CYP2E1 970	inhibitor 3277 Sources: https://jpet.aspetjournals.org/content/297/3/1166 Page: -	no
CYP2E1 970	inhibitor 3277 Sources: https://www.ema.europa.eu/en/documents/assessment-report/teysuno-epar-public-assessment-report_en.pdf#page=18 Page: 18.0	no
CYP3A4 1925	inhibitor 3277 Sources: https://jpet.aspetjournals.org/content/297/3/1166 Page: -	no
CYP2B6 1001	inducer 1573 Sources: https://www.ema.europa.eu/en/documents/assessment-report/teysuno-epar-public-assessment-report_en.pdf#page=18 Page: 18.0	weak
CYP2C8 965	inducer 1573 Sources: https://www.ema.europa.eu/en/documents/assessment-report/teysuno-epar-public-assessment-report_en.pdf#page=18 Page: 18.0	weak
CYP3A4/5 335	inducer 1573 Sources: https://www.ema.europa.eu/en/documents/assessment-report/teysuno-epar-public-assessment-report_en.pdf#page=18 Page: 18.0	weak
CYP2C9 1819	supressor 155 Sources: https://onlinelibrary.wiley.com/doi/full/10.1111/j.1742-7843.2006.pto_304.x Page: -	yes

Drug as victim

Target	Modality	Activity
CYP2A6 543	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/11106261/ Page: -	major
CYP2C9 1037	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/11106261/ Page: -	major
CYP1A1 349	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/11106261/ Page: -	minor
CYP1A2 1054	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/11106261/ Page: -	minor
CYP2B6 664	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/11106261/ Page: -	no
CYP2C19 991	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/11106261/ Page: -	no
CYP2D6 1217	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/11106261/ Page: -	no
CYP3A4 1737	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/11106261/ Page: -	no
CYP2C8 693	substrate 3367 Sources: https://europepmc.org/article/med/11095583 Page: -	yes
CYP2E1 667	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/11106261/ Page: -	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1647	inhibitor 1626 Sources: https://www.ema.europa.eu/en/documents/assessment-report/teysuno-epar-public-assessment-report_en.pdf#page=15 Page: -

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY41650	https://www.001chemical.com/chem/51-21-8
3B Scientific (Wuhan) Corp	3B3-000071	http://www.3bsc.com/index/pro_info.php?id=21959
AA Blocks	AA003MP2	http://www.aablocks.com/goods/Goods/detail?id=AA003MP2
AEchem Scientific Corp., USA	AE1-017093	http://www.aechemsc.com/info_products/AE1-017093.php
AHH Chemical co.,ltd	MT-00090	http://www.ahhchemical.com/product/MT-00090.html
AHH Chemical co.,ltd	MT-13743	http://www.ahhchemical.com/product/MT-13743.html
AK Scientific, Inc. (AKSCI)	67526	http://www.aksci.com/item_detail.php?cat=67526
AbMole Bioscience	M2289	http://www.abmole.com/products/adrucil.html
Acadechem	ACDS-070009	http://www.acadechemical.com/product/144708
Aceschem	ACF015286	https://www.aceschem.com/catalog/51-21-8.html
Achemica	ACMC-1ATRK	http://www.achemica.com/prodinfo/?id=19165
Achemo Scientific Limited	AC-11423	http://www.achemo.com/search/?Keyword= 51-21-8
Achemtek	0104-011005	http://www.achemtek.com/51-21-8
Acorn PharmaTech	ACN-036606	http://www.acornpharmatech.com/
Acros Organics	AC228440250	https://www.fishersci.com/shop/products/5-fluorouracil-99-acros-organics-2/AC228440250
Acros Organics	AC228441000	https://www.fishersci.com/shop/products/5-fluorouracil-99-acros-organics-3/AC228441000
Acros Organics	AC228440010	https://www.fishersci.com/shop/products/5-fluorouracil-99-acros-organics/AC228440010
Acros Organics	AC228440050	https://www.fishersci.com/shop/products/5-fluorouracil-99-acros-organics/AC228440050
Adooq BioScience	Fluorouracil - Adrucil	http://www.adooq.com/fluorouracil-adrucil.html
Adooq BioScience	A10042	https://www.adooq.com/fluorouracil-adrucil.html
Alfa Aesar	A13456	https://www.alfa.com/en/catalog/A13456/
Alfa Chemistry	AP51218	https://reagents.alfa-chemistry.com/product/5-fluorouracil-cas-51-21-8-12276.html
Alfa Chemistry	AP51218-A	https://reagents.alfa-chemistry.com/product/fluorouracil-cas-51-21-8-12279.html
Alichem	490004810	http://www.alichem.com/en/products/51-21-8.html
Allbio Pharm Co., Ltd	AD04457	http://www.allbiopharm.com/product/n/AD04457
Ambinter	Amb19132363	http://www.ambinter.com/reference/19132363
Ambinter	Amb19392163	http://www.ambinter.com/reference/19392163
Anward	ANW-31214	http://www.anward.com/pro_result/19403
ApexBio Technology	A4071	http://www.apexbt.com/fluorouracil-adrucil.html
Ark Pharm	AK-46307	http://www.arkpharminc.com/products/51-21-8.html
Aromalake	LS40596	http://www.aromalake.com/5-Fluorouracil-p3117.html
AstaTech, Inc.	28568	http://www.astatechinc.com/CPSResult.php?CRNO=942
Aurora Fine Chemicals LLC	A00.150.701	http://online.aurorafinechemicals.com/info?ID=A00.150.701
Aurora Fine Chemicals LLC	K00.351.222	http://online.aurorafinechemicals.com/info?ID=K00.351.222
Aurum Pharmatech LLC	W-5036	http://www.Aurumpharmatech.com/Product/ProductDetails/W_5036
AvaChem Scientific	6034	https://www.avachem.com/productSearch.asp?6034
BLD Pharm	BD9397	http://www.bldpharm.com/products/51-21-8.html
BOC Sciences	68941-95-7	https://www.bocsci.com/5-fluorouracil-15n2-cas-68941-95-7-item-212668.html
BioChemPartner	BCP02083	http://www.biochempartner.com/51-21-8-BCP02083
BioCrick	BCC2135	http://www.biocrick.com/Fluorouracil-Adrucil-BCC2135.html
BioSynth	W-202929	https://www.biosynth.com/en/products/chemical-intermediates/advanced-intermediates/products/W-202929.html
Boerchem	BC227022	http://www.boerchem.com/?product_38260.html
BroadPharm	W-60379	https://www.broadpharm.com/web/product.php?catalog=W-60379
CSNpharm	CSN19496	https://www.csnpharm.com/products/5-fluorouracil.html
Calbiochem	343922	http://www.emdbiosciences.com/product/343922
Chem Scene	CS-0993	http://www.chemscene.com/51-21-8.html
ChemFish Tokyo co.,ltd	3385	http://www.chemfish.co.jp/index.php?id=4571&project=product
ChemMol	1201418	http://www.chemmol.com/chemmol/1201418.html
ChemMol	30101108	http://www.chemmol.com/chemmol/30101108.html
ChemMol	42306771	http://www.chemmol.com/chemmol/42306771.html
ChemMol	44008012	http://www.chemmol.com/chemmol/44008012.html
ChemMol	49401699	http://www.chemmol.com/chemmol/49401699.html
Chemenu	CM110233	http://www.chemenu.com/products/CM110233
Chemspace	CSSB00000198969	https://chem-space.com/CSSB00000198969
Clearsynth	CS-EB-00905	https://www.clearsynth.com/en/CSEB00905.html
Clearsynth	CS-ER-00897	https://www.clearsynth.com/en/CSER00897.html
Clearsynth	CS-R-00260	https://www.clearsynth.com/en/CSR00260.html
Clearsynth	CS-T-54940	https://www.clearsynth.com/en/CST54940.html
DC Chemicals	DC8944	http://www.dcchemicals.com/product_show-5_Fluorouracil.html
Debye Scientific	DB-065735	http://www.debyesci.com/cas_191047-65-1.html
Debye Scientific	DB-051923	http://www.debyesci.com/cas_51-21-8.html
EMD Millipore	343922	http://www.emdbiosciences.com/product/343922
Enamine	Z275128052	https://www.enaminestore.com/catalog/Z275128052
Finetech	FT-0707652	http://www.finetechnology-ind.com/prod/detail/pub/191047-65-1.html
Finetech	FT-0695667	http://www.finetechnology-ind.com/prod/detail/pub/23935-92-4.html
Finetech	FT-0601511	http://www.finetechnology-ind.com/prod/detail/pub/51-21-8.html
Finetech	FT-0695666	http://www.finetechnology-ind.com/prod/detail/pub/766-63-2.html
Finetech	FT-0668745	http://www.finetechnology-ind.com/prod/detail/pub/90344-84-6.html
FondChemical	FDB-2824	http://www.fondchemical.com/cpshow_cid_8_pid_2111.html
Glentham Life Sciences	GP6168	http://www.glentham.com/products/product/GP6168/
Hairui	HR126763	http://www.hairuichem.com/en/product/51-21-8.html
LGC Standards	LGCFOR0593.00	https://www.lgcstandards.com/US/en/p/LGCFOR0593.00
LGC Standards	MM0593.00-0250	https://www.lgcstandards.com/US/en/p/MM0593.00-0250
Lab Network	LN00115439	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN00115439
Matrix Scientific	5763	https://www.matrixscientific.com/005763.html
MedChem Express	HY-90006	https://www.medchemexpress.com/5-Fluorouracil.html
Molcore	MC41650	https://www.molcore.com/product/51-21-8
MuseChem	I003837	https://www.musechem.com/product/I003837.html
MuseChem	M034650	https://www.musechem.com/product/M034650.html
MuseChem	M035002	https://www.musechem.com/product/M035002.html
MuseChem	M042762	https://www.musechem.com/product/M042762.html
OChem	3062	http://www.ocheminc.com/index.php?act=psearch&pid=51F218
Oakwood	3241	http://www.oakwoodchemical.com/ProductsList.aspx?CategoryID=-2&txtSearch=1295&ExtHyperLink=1
Parchem	28079	http://www.parchem.com/chemical-supplier-distributor/5-Fluorouracil-018079.aspx
Parchem	28989	http://www.parchem.com/chemical-supplier-distributor/Fluorouracil-018989.aspx
Parchem	28990	http://www.parchem.com/chemical-supplier-distributor/Fluorouracil-018990.aspx
Renno Tech	RP19888	http://www.rennotech.com/product_show.asp?id=25639
Selleck Chemicals	S1209	http://www.selleckchem.com/products/Adrucil(Fluorouracil).html
Shanghai Send Pharmaceutical Technology Co., Ltd	send36392	http://shsendpharm.com/
Sigma-Aldrich	858471_ALDRICH	https://www.sigmaaldrich.com/catalog/product/aldrich/858471?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Sigma-Aldrich	03738_SIAL	https://www.sigmaaldrich.com/catalog/product/sial/03738?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Sigma-Aldrich	04541_SIAL	https://www.sigmaaldrich.com/catalog/product/sial/04541?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Sigma-Aldrich	BP995_SIAL	https://www.sigmaaldrich.com/catalog/product/sial/bp995?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Sigma-Aldrich	1279000_USP	https://www.sigmaaldrich.com/catalog/product/usp/1279000?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Sinfoo Biotech	S054352	http://www.sinfoobiotech.com/product/1057750
Smolecule	S528186	http://www.smolecule.com/products/s528186
Smolecule	S748664	https://www.smolecule.com/products/s748664
TCI (Tokyo Chemical Industry)	F0151	http://www.tcichemicals.com/eshop/en/us/commodity/F0151/index.html
THE BioTek	bt-268348	https://www.thebiotek.com/product/inhibitors/bt-268348
Tocris	3257	https://www.tocris.com/products/5-fluorouracil_3257
TripleBond	CF0033	http://www.triplebond-canada.com/prod/657/
Vitas-M Laboratory	BBL009635	http://www.request.vitasmlab.biz/index.php?option=com_search_stk&Itemid=22&stk=BBL009635&?utm_source=pubchem&utm_medium=p_search_link&utm_campaign=pubchem_search&utm_content=pubchem_slink
VladaChem	VL142454	https://www.vladachem.com/product.php?products=51-21-8
VladaChem	VL163075	https://www.vladachem.com/product.php?products=51-21-8
VladaChem	VL265757-100G	https://www.vladachem.com/product.php?products=51-21-8
Yuhao Chemical	RT16644	http://www.chemyuhao.com/51-21-8.html
abcr GmbH	AB116873	http://www.abcr.com/shop/en/AB116873
eNovation Chemicals	K09113	http://www.enovationchem.com/productDetails.asp?productID=K09113
eNovation Chemicals	D378290	https://www.enovationchem.com/ProductDetails.asp?ProductID=D378290
mcule	MCULE-6338086431	https://mcule.com/MCULE-6338086431/

PubMed

Title	Date	PubMed
Studies of antitumor agents. 1. Resolution of racemic 1-(tetrahydro-2-furanyl)-k-fluorouracil into the R and S isomers and examination of the biological activities of the isomers.	1977 Dec	338900
[Experience of a combination chemotherapy consisting of 5-FU, MMC, and FT-207--side effects against kidney].	1983 Sep	6412636
[A case of variant angina induced by 5-fluorouracil and Tegafur].	1988 Nov	3150118
[Macrocytic anemia as a possible adverse effect of fluoropyrimidines].	1990 Aug	2117887
Hypercoagulopathy induced by chemotherapy in a patient with lung cancer. A possible role for a factor with thrombosis-inducing activity (TIA).	1992 Jan	1729088
Leukoencephalopathy induced by chemotherapy with tegafur, a 5-fluorouracil derivative.	1998 Nov	9829818
Moderate neutropenia with adjuvant CMF confers improved survival in early breast cancer.	2003 Nov 17	14612889
The potential for oral combination chemotherapy of 5'-deoxy-5-fluorouridine, a 5-FU prodrug, and cyclophosphamide for metastatic breast cancer.	2003 Nov 3	14583760
Comparative pharmacology of oral fluoropyrimidines: a focus on pharmacokinetics, pharmacodynamics and pharmacomodulation.	2004 Aug 16	15280932
p53 and VEGF expression are independent predictors of tumour recurrence and survival following curative resection of gastric cancer.	2004 Jan 12	14710231
Dependence of chemotherapy response on p53 mutation status in a panel of human cancer lines maintained in nude mice.	2004 Jun	15182437
Severe colitis after administration of UFT chemotherapy for temporal bone carcinoma.	2004 Mar	15006714
Phase I trial of UFT/leucovorin and irinotecan in patients with advanced cancer.	2004 Mar	14962716
Adjuvant immunochemotherapy with oral Tegafur/Uracil plus PSK in patients with stage II or III colorectal cancer: a randomised controlled study.	2004 Mar 8	14997197
Neurotoxic effects of alpha-fluoro-beta-alanine (FBAL) and fluoroacetic acid (FA) on dogs.	2004 May	15206584
Postoperative chemotherapy for non-small cell lung cancer: A systematic review and meta-analysis.	2004 Sep	15354101
New medium oxacyclic O,N-acetals and related open analogues: biological activities.	2005	15974993
Phase I trial of Orzel (UFT plus leucovorin), cisplatin, and radiotherapy in the treatment of potentially resectable esophageal cancer.	2005 Apr 1	15817338
Identification of molecular mechanisms for cellular drug resistance by combining drug activity and gene expression profiles.	2005 Aug 22	16012520
Antitumoural properties of benzannelated seven-membered 5-fluorouracil derivatives and related open analogues. Molecular markers for apoptosis and cell cycle dysregulation.	2005 Feb	15752467
UFT plus gemcitabine combination chemotherapy in patients with advanced non-small-cell lung cancer: a multi-institutional phase II trial.	2005 Oct 3	16175186
Cyp2a6 is a principal enzyme involved in hydroxylation of 1,7-dimethylxanthine, a main caffeine metabolite, in humans.	2005 Sep	15980104
[Thymidylate synthase gene promoter polymorphism in patients with advanced head and neck cancer treated by radio- and 5-fluorouracil chemotherapy].	2006	16617381
Time-related improvement of survival in resectable gastric cancer: the role of Japanese-style gastrectomy with D2 lymphadenectomy and adjuvant chemotherapy.	2006 Aug 11	16904003
'A phase II study of oral uracil/ftorafur (UFT) plus leucovorin combined with oxaliplatin (TEGAFOX) as first-line treatment in patients with metastatic colorectal cancer'.	2006 Jan 16	16404362
An open, multi-centre, phase II clinical trial to evaluate the efficacy and safety of paclitaxel, UFT, and leucovorin in patients with advanced gastric cancer.	2006 Jul 17	16804524
An individual patient data meta-analysis of adjuvant therapy with uracil-tegafur (UFT) in patients with curatively resected rectal cancer.	2007 Apr 23	17375049
Reflections on adjuvant treatment of gastric cancer.	2007 Aug	18472977
Phase II study of UFT with leucovorin and irinotecan (TEGAFIRI): first-line therapy for metastatic colorectal cancer.	2007 Aug 6	17637682
A phase I/II study of irinotecan when added to 5-fluorouracil and leucovorin and pelvic radiation in locally advanced rectal cancer: a Colorectal Clinical Oncology Group Study.	2007 Feb 26	17262086
Ftorafur loading and controlled release from poly(ethyl-2-cyanoacrylate) and poly(butylcyanoacrylate) nanospheres.	2007 Jun 7	17223292
5-Fluorouracil incorporated into the tissue RNA of human and rat bladder carcinoma after administration of 1-(2-tetrahydrofuryl)-5-fluorouracil combined with uracil.	2008 Apr	18463958
The CYP2A6*4 allele is determinant of S-1 pharmacokinetics in Japanese patients with non-small-cell lung cancer.	2008 Apr	18212800
Dihydropyrimidine dehydrogenases and cytidine-deaminase gene polymorphisms as outcome predictors in resected gastric cancer patients treated with fluoropyrimidine adjuvant chemotherapy.	2008 Aug 1	18537153
Novel prodrugs of tegafur that display improved anticancer activity and antiangiogenic properties.	2008 Jan 24	18163551
[Study on antitumor effect and its toxicity of Ipomoea Batatas Poir Cv anthocyanins].	2008 Jul	18839539
Study of carbonyl iron/poly(butylcyanoacrylate) (core/shell) particles as anticancer drug delivery systems Loading and release properties.	2008 Mar 3	18249100
A phase II study of UFT with leucovorin administered as a twice daily schedule in the treatment of patients with metastatic colorectal cancer.	2008 Sep 2	18728662
Role of oxaliplatin in the treatment of colorectal cancer.	2009 Feb	19436599
Development history and concept of an oral anticancer agent S-1 (TS-1): its clinical usefulness and future vistas.	2009 Jan	19052037
Complete remission of platinium refractory ovarian cancer with second line tegafur with uracil monotherapy: a case report.	2009 Mar	18504578
Analysis of feasibility and toxicity of concurrent chemoradiotherapy with S-1 for locally advanced squamous cell carcinoma of the head and neck in elderly cases and/or cases with comorbidity.	2009 Oct	19219603
Two dosages of oral fluoropyrimidine S-1 of 35 and 40 mg/m2 bid: comparison of the pharmacokinetic profiles in Korean patients with advanced gastric cancer.	2010 Jan	19880858
Formulation and physicochemical characterization of poly(epsilon-caprolactone) nanoparticles loaded with ftorafur and diclofenac sodium.	2010 Jan 1	19740632
[Dihydropyrimidine dehydrogenase deficiency and toxicity to fluoropyrimidine].	2010 Jan-Feb	20146975
A phase 2 study of a fixed combination of uracil and ftorafur (UFT) and leucovorin given orally in a 3-times-daily regimen to treat patients with recurrent metastatic breast cancer.	2010 Mar 15	20091835
A phase 2 study of a fixed combination of uracil and ftorafur and leucovorin given orally in a twice-daily regimen to treat patients with recurrent metastatic breast cancer.	2010 May 15	20225231
Adenoviral delivery of pan-caspase inhibitor p35 enhances bystander killing by P450 gene-directed enzyme prodrug therapy using cyclophosphamide+.	2010 Sep 13	20836875
Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2.	2011 Jul 14	21599003
Zebrafish (Danio rerio) embryos as a model for testing proteratogens.	2011 Mar 15	21237239

Patents

Sample Use Guides

In Vivo Use Guide

General dosage regimen (for adults): UFT (Tegafur, urac) is administered 1.5-3g (equivalent to 300-600 mg of Tegafur) daily in two to three divided doses. For uterine cervical cancer, UFT is administered 3g (equivalent to 600mg of Tegafur) daily in two to three divided doses

Route of Administration: Oral

In Vitro Use Guide

Unknown

Substance Class	Chemical Created by `admin` on `Fri Dec 15 15:03:25 GMT 2023` Edited by `admin` on `Fri Dec 15 15:03:25 GMT 2023`
Record UNII	1548R74NSZ
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

TEGAFUR

Official Name

English

tegafur [INN]

Common Name

English

TEGAFUR COMPONENT OF TEYSUNO

Brand Name

English

TEGAFUR [USAN]

Common Name

English

5-FLUORO-1-(TETRAHYDRO-2-FURYL)-URACIL

Systematic Name

English

FURAFLUOR

Brand Name

English

TEGAFUR [JAN]

Common Name

English

FULFEEL

Brand Name

English

Tegafur [WHO-DD]

Common Name

English

ATILLON

Brand Name

English

LAMAR

Brand Name

English

TEGAFUR [EMA EPAR]

Common Name

English

SUNFURAL

Brand Name

English

EXONAL

Brand Name

English

TEGAFUR [MI]

Common Name

English

RIOL

Brand Name

English

NEBERK

Brand Name

English

TEFSIEL C

Brand Name

English

2,4(1H,3H)PYRIMIDINEDIONE, 5-FLUORO-1-(TETRAHYDRO-2-FURANYL)-

Systematic Name

English

SINOFLUROL

Brand Name

English

TEYSUNO COMPONENT TEGAFUR

Brand Name

English

FUROFUTRAN

Brand Name

English

COPAROGIN

Brand Name

English

FULAID

Brand Name

English

FUTRAFUL

Brand Name

English

LIFRIL

Brand Name

English

NITOBANIL

Brand Name

English

MJF-12264

Code

English

CITOFUR

Brand Name

English

FTORAFUR

Brand Name

English

FENTAL

Brand Name

English

FRANROSE

Brand Name

English

NSC-148958

Code

English

FT-207

Code

English

TEGAFUR [MART.]

Common Name

English

Classification Tree Code System Code

WHO-ATC

L01BC53