Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C20H23N7O6 |
Molecular Weight | 457.4399 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
NC1=NC(=O)C2=C(NC[C@@H]3CN(CN23)C4=CC=C(C=C4)C(=O)N[C@@H](CCC(O)=O)C(O)=O)N1
InChI
InChIKey=QYNUQALWYRSVHF-OLZOCXBDSA-N
InChI=1S/C20H23N7O6/c21-20-24-16-15(18(31)25-20)27-9-26(8-12(27)7-22-16)11-3-1-10(2-4-11)17(30)23-13(19(32)33)5-6-14(28)29/h1-4,12-13H,5-9H2,(H,23,30)(H,28,29)(H,32,33)(H4,21,22,24,25,31)/t12-,13+/m1/s1
Molecular Formula | C20H23N7O6 |
Molecular Weight | 457.4399 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
METHYLENETETRAHYDROFOLIC ACID, L-(+), an endogenous biomodulator that was developed under the brand name modufolin or arfolitixorin by the Isofol Medical. Arfolitixorin is developed to increase the efficacy of standard of care chemotherapy for advanced colorectal cancer. This drug is currently being studied in a global phase 3 clinical trial. Besides, the drug successfully completed phase II as rescue therapy for osteosarcoma. 21 May 2019 Isofol Medical has received clinical patent protection for the arfolitixorinin USA. It relates to a method of increasing blood concentration of deoxyuridine, a blood biomarker for inhibition of tumor growth in human cancer treatment.
Approval Year
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2860 ng/mL |
30 mg/m² single, intravenous dose: 30 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: FLUOROURACIL |
METHYLENETETRAHYDROFOLIC ACID, L-( )- plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
4410 ng/mL |
60 mg/m² single, intravenous dose: 60 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: FLUOROURACIL |
METHYLENETETRAHYDROFOLIC ACID, L-( )- plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
21200 ng/mL |
240 mg/m² single, intravenous dose: 240 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: FLUOROURACIL |
METHYLENETETRAHYDROFOLIC ACID, L-( )- plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
39.4 pmol/mL |
416 μg/m² single, intravenous dose: 416 μg/m² route of administration: Intravenous experiment type: SINGLE co-administered: FLUOROURACIL |
METHYLENETETRAHYDROFOLIC ACID, L-( )- plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1460 ng × h/mL |
30 mg/m² single, intravenous dose: 30 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: FLUOROURACIL |
METHYLENETETRAHYDROFOLIC ACID, L-( )- plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
2370 ng × h/mL |
60 mg/m² single, intravenous dose: 60 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: FLUOROURACIL |
METHYLENETETRAHYDROFOLIC ACID, L-( )- plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
10600 ng × h/mL |
240 mg/m² single, intravenous dose: 240 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: FLUOROURACIL |
METHYLENETETRAHYDROFOLIC ACID, L-( )- plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
210 pmol × h/mL |
416 μg/m² single, intravenous dose: 416 μg/m² route of administration: Intravenous experiment type: SINGLE co-administered: FLUOROURACIL |
METHYLENETETRAHYDROFOLIC ACID, L-( )- plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
PubMed
Title | Date | PubMed |
---|---|---|
Molecular biology of 5,10-methylenetetrahydrofolate reductase. | 2000 Jan-Feb |
|
Formaldehyde-detoxifying role of the tetrahydromethanopterin-linked pathway in Methylobacterium extorquens AM1. | 2003 Dec |
|
Phase 1 dose de-escalation trial of the endogenous folate [6R]-5,10-methylene tetrahydrofolate in combination with fixed-dose pemetrexed as neoadjuvant therapy in patients with resectable rectal cancer. | 2015 Oct |
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT02244632
IV injection every second week for 8 weeks 30 to 240 mg/m2
Route of Administration:
Intravenous
Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 21:34:58 GMT 2025
by
admin
on
Mon Mar 31 21:34:58 GMT 2025
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Record UNII |
Z8R4A37V9Q
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Record Status |
Validated (UNII)
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FDA ORPHAN DRUG |
189304
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1989
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DB12676
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FG-126
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C157079
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135398645
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Related Record | Type | Details | ||
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SALT/SOLVATE -> PARENT | |||
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SALT/SOLVATE -> PARENT |
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ACTIVE MOIETY |