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5Fluorouracil

Phase 3

Metastatic Colorectal Cancer | Small molecule | Oncology |Merck KGaA|Last Updated: Jan 28, 2020

Target and mechanism

Molecular targetTYMS
Target classInhibitor
ModalitySmall molecule
ChEMBLCHEMBL185

Also known as 5-fluorouracil (5-FU), 5-fluorouracil

Success Probability

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Market & Valuation

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Trial Design

RandomizedACTIVE_CONTROLLEDDMC
Total Trials1
Total Enrollment553

FDA Designations

No designations recorded

Clinical trial landscape

5Fluorouracil · 1 trial · 1 indication

Phase 3 1
NCT01228734A Trial to Compare Oxaliplatin, Folinic Acid (FA) and 5-Fluorouracil (5FU) Combination Chemotherapy (FOLFOX-4) With or Without Cetuximab in the 1st Line Treatment of Metastatic Colorectal Cancer (mCRC) in Chinese Rat Sarcoma Viral Oncogene Homolog (RAS) Wild-type PatientsMetastatic Colorectal Cancer
COMPLETED553 Analytics
PHASE3COMPLETED
A Trial to Compare Oxaliplatin, Folinic Acid (FA) and 5-Fluorouracil (5FU) Combination Chemotherapy (FOLFOX-4) With or Without Cetuximab in the 1st Line Treatment of Metastatic Colorectal Cancer (mCRC) in Chinese Rat Sarcoma Viral Oncogene Homolog (RAS) Wild-type Patients
Metastatic Colorectal CancerUnlock trial analytics

Study Endpoints

Primary Endpoints

Progression Free Survival (PFS) Time
Baseline up to 333 weeks

PFS was defined as the duration (in months) from randomization until the first progressive disease (PD) observation as assessed by the Independent Review Committee (IRC) according to Response Evaluation Criteria for Solid Tumors (RECIST) version 1.0, or death due to any cause when death occurred within 90 days of randomization or the last tumor assessment, whichever was later. PD was defined as at least a 20% increase in the sum of longest diameter (LD) of the target lesions, taking as references the smallest sum LD since the treatment started (including baseline), or appearance of one or more new lesions, and/or unequivocal progression of existing non-target lesions.

Secondary Endpoints

Overall Survival (OS) Time
Baseline up to 333 weeks
Best Overall Response Rate (ORR)
Baseline up to 333 weeks
Time to Treatment Failure (TTF)
Baseline up to 333 weeks
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Study Design & Arms

AllocationRANDOMIZED
MaskingNONE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Cetuximab + FOLFOX-4EXPERIMENTALSubjects received cetuximab in combination with FOLFOX-4 chemotherapy regimen. FOLFOX-4 chemotherapy regimen consists of a combination of oxaliplatin with 5-fluorouracil (5-FU)/folinic acid (FA). Cetuximab was always administered every 7 days with an initial dose of 400 milligram per square meter (mg/m\^2) at 5 milligram per minute (mg/min) and 250 mg/m\^2 at 10 mg/min for subsequent infusions, followed by oxaliplatin 85 mg/m\^2 infused over 120 minutes at least 1 hour later. Following completion of the oxaliplatin infusion or simultaneously with oxaliplatin, FA was administered at a dose of 200 mg/m\^2 infused over 120 minutes, on Day 1, Day 2, and every 2 weeks and then 5- FU was administered as a bolus of 400 mg/m\^2/day intravenously over 2-4 minutes followed by 600 mg/m\^2/day infused over 22 hours, on Day 1, Day 2, and every 2 weeks. All subjects received treatment until progression of disease, withdrawal of consent, or unacceptable toxicity.
FOLFOX-4ACTIVE_COMPARATORSubjects received FOLFOX-4 chemotherapy regimen that consists of a combination of oxaliplatin with 5-FU/FA. Oxaliplatin 85 mg/m\^2 infused over 120 minutes was administered first or simultaneously with FA at a dose of 200 mg/m\^2 infused over 120 minutes on Day 1, Day 2, and every 2 weeks and then 5-FU was administered as a bolus of 400 mg/m\^2/day intravenously over 2-4 minutes followed by 600 mg/m\^2/day infused over 22 hours on Day 1, Day 2, and every 2 weeks. All subjects received treatment until progression of disease, withdrawal of consent, or unacceptable toxicity.

Interventions

NameTypeDescription
CetuximabDRUGCetuximab was administered every 7 days at an initial dose of 400 milligram per square meter (mg/m\^2) at 5 milligram per minute (mg/min) and 250 mg/m\^2 at 10 mg/min for subsequent infusions until progression of disease, withdrawal of consent, or unacceptable toxicity to cetuximab.
OxaliplatinDRUGOxaliplatin 85 mg/m\^2 infusion over 120 minutes on Day 1, Day 2, and then every 2 weeks until progression of disease, withdrawal of consent, or unacceptable toxicity.
Folinic AcidDRUGFA 200 mg/m\^2 infusion over 120 minutes on Day 1, Day 2, and then every 2 weeks until progression of disease, withdrawal of consent, or unacceptable toxicity.
5FluorouracilDRUG5-FU as a bolus of 400 mg/m\^2/day intravenously over 2-4 minutes followed by 600 mg/m\^2/day infusion over 22 hours on Day 1, Day 2, and then every 2 weeks until progression of disease, withdrawal of consent, or unacceptable toxicity.
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Eligibility Criteria

Age Range18 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites25

Inclusion Criteria: * Signed written informed consent (first and second) * Chinese with Chinese citizenship * Male or female subjects greater than or equal to (\>=) 18 years of age * Medically accepted effective contraception if procreative potential exists (applicable for both male and female subj...

Countries:China
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Competitive Landscape -Colorectal Cancer 258 trials (matched to "Metastatic Colorectal Cancer")

Frequently asked questions about 5Fluorouracil

What is 5-Fluorouracil used for?

5-Fluorouracil is used in the treatment of squamous cell carcinoma of the head and neck and metastatic colorectal cancer. It is an oncology small molecule that has been studied in combination with other chemotherapy agents and targeted therapies for these indications.

What does 5-Fluorouracil target?

5-Fluorouracil is a small molecule that interferes with DNA synthesis by inhibiting thymidylate synthase, an enzyme necessary for the production of thymidine nucleotides. This action disrupts cancer cell replication and is used in the treatment of head and neck cancer and metastatic colorectal cancer.

Who makes 5-Fluorouracil?

5-Fluorouracil is developed by Merck KGaA, a company traded under the ticker MKGAF. The drug is being investigated in clinical trials for oncology indications, including squamous cell carcinoma of the head and neck and metastatic colorectal cancer.

What phase is 5-Fluorouracil in?

5-Fluorouracil is in Phase 3 clinical development. It is an investigational drug being studied in completed Phase 3 trials for head and neck cancer and metastatic colorectal cancer. It has not been reported as approved for these indications in the available trial data.

What clinical trials is 5-Fluorouracil in?

5-Fluorouracil has been studied in completed trials including NCT01177956, a Phase 3 trial in recurrent or metastatic squamous cell carcinoma of the head and neck, and NCT01228734, a Phase 3 trial in metastatic colorectal cancer. These trials evaluated 5-FU in combination with other agents.

Is 5-Fluorouracil the same as 5-FU?

Yes, 5-Fluorouracil is also known as 5-FU. The abbreviation 5-FU is commonly used in clinical trial titles and medical literature to refer to the same drug, as seen in trials combining it with cetuximab and other chemotherapy agents.