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Chemistry

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Also known as: Fluciclovine f-18, Axumin, 222727-39-1, Fluciclovine f 18, Facbc, Fluciclovine f18
Molecular Formula
C5H8FNO2
Molecular Weight
132.12  g/mol
InChI Key
NTEDWGYJNHZKQW-KWCOIAHCSA-N
FDA UNII
38R1Q0L1ZE

UNII-38R1Q0L1ZE
Fluciclovine F18 is a radiotracer containing a synthetic amino acid analogue of L-leucine radiolabeled with fluorine F 18 with potential diagnostic imaging use. Similar to most amino acids, fluciclovine F18 appears to enter cells through the energy-independent L-type amino acid transporter (LAT) system. As an amino acid analogue, this agent is preferentially accumulated by tumor cells due to their increased metabolic needs; however, unlike naturally occurring amino acids, this non-natural amino acid-analogue radiotracer is not metabolized. Accordingly, fluciclovine F18 accumulates in tumor cells and can potentially be used to image tumors using positron emission tomography (PET).
Fluciclovine f-18 is a Radioactive Diagnostic Agent. The mechanism of action of fluciclovine f-18 is as a Positron Emitting Activity.
1 2D Structure

UNII-38R1Q0L1ZE

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
1-amino-3-(18F)fluoranylcyclobutane-1-carboxylic acid
2.1.2 InChI
InChI=1S/C5H8FNO2/c6-3-1-5(7,2-3)4(8)9/h3H,1-2,7H2,(H,8,9)/i6-1
2.1.3 InChI Key
NTEDWGYJNHZKQW-KWCOIAHCSA-N
2.1.4 Canonical SMILES
C1C(CC1(C(=O)O)N)F
2.1.5 Isomeric SMILES
C1C(CC1(C(=O)O)N)[18F]
2.2 Other Identifiers
2.2.1 UNII
38R1Q0L1ZE
2.3 Synonyms
2.3.1 MeSH Synonyms

1. (18f)ge-148

2. (1r,3r)-1-amino-3(18f)fluorocyclobutane-1-carboxylic Acid

3. 1-amino-3-fluorocyclobutane-1-carboxylic Acid

4. Anti-(18f)facbc

5. Axumin

6. Cyclobutanecarboxylic Acid, 1-amino-3-(fluoro-18f)-, Trans-

7. F(18)-facbc

8. F(18)1-amino-3-fluorocyclobutane-1-carboxylic Acid

9. F-facbc

10. Fluciclovine F 18

11. Fluciclovine F-18

12. Ge-148 (18f)

13. Ge-148 F-18

14. Nmk 36

15. Nmk-36

16. Nmk36 Cpd

2.3.2 Depositor-Supplied Synonyms

1. Fluciclovine F-18

2. Axumin

3. 222727-39-1

4. Fluciclovine F 18

5. Facbc

6. Fluciclovine F18

7. Nmk36

8. Ge-148

9. (18f)fluciclovine

10. Fluciclovine (18f) [inn]

11. Nmk-36

12. (18f)ge-148

13. Ge-148 F-18

14. Ge-148 (18f)

15. (18f)facbc

16. Facbc F-18

17. 38r1q0l1ze

18. Anti-1-amino-3-(18f)fluorocyclobutane-1-carboxylic Acid

19. (1r,3r)-1-amino-3(18f)fluorocyclobutane-1-carboxylic Acid

20. [18f]fluciclovine

21. [18f]facbc

22. Fluciclovine (18f) (inn)

23. 1-amino-3-(18f)fluoranylcyclobutane-1-carboxylic Acid

24. Cyclobutanecarboxylic Acid, 1-amino-3-(fluoro-18f)-, Trans-

25. Anti-(18f)fabc

26. Fluciclovine F18 [usan]

27. Anti-1-amino-3-[18f]fluorocyclobutane-1-carboxylic Acid

28. Unii-38r1q0l1ze

29. Fluciclovine ((sup 18)f)

30. Fluciclovine-f18

31. Moli001120

32. Fluciclovine ((sup 18)f) [inn]

33. Axumin (tn)

34. Nmk36 Cpd

35. Anti-[18f]facbc

36. Syn-3-[18f]facbc

37. Fluciclovine F-18 (usan)

38. Chembl254468

39. Chembl447701

40. Nmk 36

41. Schembl10017245

42. Schembl11939897

43. Schembl11939900

44. Chebi:134703

45. Dtxsid601027796

46. Fluciclovine (18f) [mi]

47. Fluciclovine F 18 [usan]

48. Bcp24384

49. Axumincn Facbccn Fluciclovine (18f)cn Ge 148cn Nmk 36

50. At31246

51. Db13146

52. Fluciclovine (18f) [who-dd]

53. Fluciclovine F-18 [orange Book]

54. D10860

55. F(18)1-amino-3-fluorocyclobutane-1-carboxylic Acid

56. Q25313613

57. Syn-1-amino-3-[18f]fluorocyclobutane-1-carboxylic Acid

58. Anti-3[18f] Facbc;f18; Anti-1-amino-3-18f-fluorocyclobutane-1-carboxylic Acid (facbc)

2.4 Create Date
2005-03-27
3 Chemical and Physical Properties
Molecular Weight 132.12 g/mol
Molecular Formula C5H8FNO2
XLogP3-2.6
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count4
Rotatable Bond Count1
Exact Mass132.056441 g/mol
Monoisotopic Mass132.056441 g/mol
Topological Polar Surface Area63.3 Ų
Heavy Atom Count9
Formal Charge0
Complexity142
Isotope Atom Count1
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Indication

Fluciclovine is indicated as a detection agent for positron emission tomography (PET) in men with suspected prostate cancer recurrence based on elevated blood prostate specific antigen (PSA) levels following prior treatment. The overexpression of L-type amino acid transporters such as LAT1 and LAT3 that mediate the uptake of essential amino acids has been extensively reported as a tumoral mechanism of cell growth.


FDA Label


This medicinal product is for diagnostic use only.

Axumin is indicated for Positron Emission Tomography (PET) imaging to detect recurrence of prostate cancer in adult men with a suspected recurrence based on elevated blood prostate specific antigen (PSA) levels after primary curative treatment.


5 Pharmacology and Biochemistry
5.1 Pharmacology

Following intravenous administration, the tumor-to-normal tissue contrast is highest between 2 and 10 minutes after injection, with a 63% reduction in mean tumor uptake at 90 minutes after injection. The scanning time point should be evaluated carefully as an early scanning can present an increased blood pool and a late scanning will translate into an increased muscle uptake. These variations should always be considered in the image interpretation.


5.2 FDA Pharmacological Classification
5.2.1 Active Moiety
FLUCICLOVINE F-18
5.2.2 FDA UNII
38R1Q0L1ZE
5.2.3 Pharmacological Classes
Radioactive Diagnostic Agent [EPC]; Positron Emitting Activity [MoA]
5.3 ATC Code

V09IX12


V - Various

V09 - Diagnostic radiopharmaceuticals

V09I - Tumour detection

V09IX - Other diagnostic radiopharmaceuticals for tumour detection

V09IX12 - Fluciclovine (18F)


5.4 Absorption, Distribution and Excretion

Absorption

After intravenous administration of fluciclovine, the major distribution happens in liver (14%), red bone marrow (12%), lung (7%), myocardium (4%) and pancreas (3%). With increasing time, the dose gets distributed into skeletal muscle.


Route of Elimination

In the first four hours post-injection, 3% of administered dose is excreted in the urine which increases to 5% after 24 hours post-injection.


Volume of Distribution

The compartmental volume of distribution of fluciclovine is in prostate 0.97 L, vesicle 0.79 L, red bone marrow 0.98 L, gluteus muscle 2.13 L and obturator muscle 2.23 L.


Clearance

Fluciclovine renal clearance and excretion is minimal.


5.5 Metabolism/Metabolites

Fluciclovine is not metabolized and it is not incorporated into newly synthesized proteins.


5.6 Biological Half-Life

Fluciclovine is a cyclotron produced radionuclide that decays by positron emission (+ decay, 96.7%) and orbital electron capture (3.3%) to stable oxygen 18 with a physical half-life of 109.7 minutes.


5.7 Mechanism of Action

Fluciclovine is transported into the prostate cancer cells via ASCT2 and LAT1 transporters. The activity of LAT1 gets increased in acidic pH, condition that is developed intra-tumorally at certain size. The uptake of fluciclovine presents an androgen-dependent dynamic in hormone sensitive cells.


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Looking for 222727-39-1 / UNII-38R1Q0L1ZE API manufacturers, exporters & distributors?

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API | Excipient name

UNII-38R1Q0L1ZE

Synonyms

Fluciclovine f-18, Axumin, 222727-39-1, Fluciclovine f 18, Facbc, Fluciclovine f18

Cas Number

222727-39-1

Unique Ingredient Identifier (UNII)

38R1Q0L1ZE

About UNII-38R1Q0L1ZE

Fluciclovine F18 is a radiotracer containing a synthetic amino acid analogue of L-leucine radiolabeled with fluorine F 18 with potential diagnostic imaging use. Similar to most amino acids, fluciclovine F18 appears to enter cells through the energy-independent L-type amino acid transporter (LAT) system. As an amino acid analogue, this agent is preferentially accumulated by tumor cells due to their increased metabolic needs; however, unlike naturally occurring amino acids, this non-natural amino acid-analogue radiotracer is not metabolized. Accordingly, fluciclovine F18 accumulates in tumor cells and can potentially be used to image tumors using positron emission tomography (PET).

UNII-38R1Q0L1ZE Manufacturers

A UNII-38R1Q0L1ZE manufacturer is defined as any person or entity involved in the manufacture, preparation, processing, compounding or propagation of UNII-38R1Q0L1ZE, including repackagers and relabelers. The FDA regulates UNII-38R1Q0L1ZE manufacturers to ensure that their products comply with relevant laws and regulations and are safe and effective to use. UNII-38R1Q0L1ZE API Manufacturers are required to adhere to Good Manufacturing Practices (GMP) to ensure that their products are consistently manufactured to meet established quality criteria.

UNII-38R1Q0L1ZE Suppliers

A UNII-38R1Q0L1ZE supplier is an individual or a company that provides UNII-38R1Q0L1ZE active pharmaceutical ingredient (API) or UNII-38R1Q0L1ZE finished formulations upon request. The UNII-38R1Q0L1ZE suppliers may include UNII-38R1Q0L1ZE API manufacturers, exporters, distributors and traders.

UNII-38R1Q0L1ZE GMP

UNII-38R1Q0L1ZE Active pharmaceutical ingredient (API) is produced in GMP-certified manufacturing facility.

GMP stands for Good Manufacturing Practices, which is a system used in the pharmaceutical industry to make sure that goods are regularly produced and monitored in accordance with quality standards. The FDA’s current Good Manufacturing Practices requirements are referred to as cGMP or current GMP which indicates that the company follows the most recent GMP specifications. The World Health Organization (WHO) has its own set of GMP guidelines, called the WHO GMP. Different countries can also set their own guidelines for GMP like China (Chinese GMP) or the EU (EU GMP).

PharmaCompass offers a list of UNII-38R1Q0L1ZE GMP manufacturers, exporters & distributors, which can be sorted by USDMF, JDMF, KDMF, CEP (COS), WC, API price, and more, enabling you to easily find the right UNII-38R1Q0L1ZE GMP manufacturer or UNII-38R1Q0L1ZE GMP API supplier for your needs.

UNII-38R1Q0L1ZE CoA

A UNII-38R1Q0L1ZE CoA (Certificate of Analysis) is a formal document that attests to UNII-38R1Q0L1ZE's compliance with UNII-38R1Q0L1ZE specifications and serves as a tool for batch-level quality control.

UNII-38R1Q0L1ZE CoA mostly includes findings from lab analyses of a specific batch. For each UNII-38R1Q0L1ZE CoA document that a company creates, the USFDA specifies specific requirements, such as supplier information, material identification, transportation data, evidence of conformity and signature data.

UNII-38R1Q0L1ZE may be tested according to a variety of international standards, such as European Pharmacopoeia (UNII-38R1Q0L1ZE EP), UNII-38R1Q0L1ZE JP (Japanese Pharmacopeia) and the US Pharmacopoeia (UNII-38R1Q0L1ZE USP).

Inform the supplier about your product requirements, specifying if you need a product with particular monograph like EP (Ph. Eur.), USP, JP, BP, or any other quality. In addition, clarify whether you need hydrochloride (HCl), anhydricum, base, micronisatum or a specific level of purity. To find reputable suppliers, utilize the filters and select those certified by GMP, FDA, or any other certification as per your requirement.
For your convenience, we have listed synonyms and CAS numbers to help you find the best supplier. The use of synonyms and CAS numbers can be helpful in identifying potential suppliers, but it is crucial to note that they might not always indicate the exact same product. It is important to confirm the product details with the supplier before making a purchase to ensure that it meets your requirements.
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