[CAS NO. 70052-12-9] Eflornithine
PRODUCTS SPECIFICATIONS [70052-12-9]
DESCRIPTION [70052-12-9]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 182.17 |
| Molecular Formula | C6H12F2N2O2 |
| SMILES | NC(CCCN)(C(F)F)C(O)=O |
9 Publications Citing Use of MCE
- [1]Sci Adv. 2023 May 19;9(20):eade0718.
- [2]JACC Basic Transl Sci. 2022 Aug 3;7(8):820-840.
- [3]Commun Biol. 2019 May 8;2:171.
- [4]Cancer Nanotechnol. 2023 May 9.
- [5]Food Biosci. 2023 Oct, 55, 102970.
- [6]Front Oncol. 2021 Mar 11;11:636373.
- [7]Oncotargets Ther. 2020 Nov 17;13:11697-11709.
- [8]RSC Adv. 2019, 9, 11026-11037.
- [9]bioRxiv. 2024 Jan 15.
Summary
Eflornithine is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase . Eflornithine is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women.
IC50 & Target
|
Trypanosoma |
In Vivo
Eflornithine is the only new molecule registered for the treatment of human African trypanosomiasis over the last 50 years. It is the drug used mainly as a back-up for melarsoprol refractory Trypanosoma brucei gambiense cases [1] . In subjects with excessive, unwanted facial hair, eflornithine 15% cream is superior to placebo in reducing hair growth. After 24 weeks' treatment, 58% of eflornithine and 34% of placebo subjects have at least some improvement in facial hirsutism [2] . The hair growth inhibitory activity of eflornithine is significantly enhanced when the eflornithine cream is applied onto a mouse skin area pretreated with microneedles [3] . Treatment of coarctation hypertensive rats with eflornithine results in a normalization of the contractile intensity to KCI and norepinephrine and relaxations to acetylcholine by 14 days of hypertension [4] .
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00006101 | Thomas E. Ahlering|National Cancer Institute (NCI)|University of California, Irvine |
Prostate Cancer
|
October 1998 | Phase 2 |
| NCT05500508 | Aminex Therapeutics, Inc. |
Cancer|Solid Tumor|Solid Carcinoma|Advanced Cancer|DIPG Brain Tumor|Ovary Cancer|Breast Cancer|Papillary Thyroid Cancer|Head and Neck Cancer|Gastric Cancer|Nsclc|Mesotheliomas Pleural|Mesothelioma Peritoneum|Esophageal Cancer|Diffuse Midline Glioma, H3 K27M-Mutant|Endometrial Cancer|Cervical Cancer|Melanoma|Colorectal Cancer|Glioma, Malignant
|
November 29, 2022 | Phase 1|Phase 2 |
| NCT02794428 | Vanderbilt-Ingram Cancer Center|National Cancer Institute (NCI)|Cancer Prevention Pharmaceuticals, Inc. |
Gastric Cancer|Gastric Intestinal Metaplasia
|
September 19, 2016 | Phase 2 |
| NCT05594563 | Emily K. Sims|Juvenile Diabetes Research Foundation|Cancer Prevention Pharmaceuticals, Inc.|Indiana University |
Type 1 Diabetes
|
March 14, 2023 | Phase 2 |
| NCT00152048 | Allergan |
Hirsutism
|
November 30, 2004 | Phase 4 |
| NCT00003076 | University of Michigan Rogel Cancer Center|National Cancer Institute (NCI) |
Esophageal Cancer
|
October 1995 | Phase 2 |
| NCT03536728 | Aminex Therapeutics, Inc. |
Cancer|Solid Tumor|Solid Carcinoma|Advanced Cancer
|
June 12, 2018 | Phase 1 |
| NCT02559778 | Wake Forest University Health Sciences|Dell, Inc.|Beat NB Cancer Foundation|K C Pharmaceuticals Inc.|Team Parker for Life |
Neuroblastoma
|
September 2015 | Phase 2 |
| NCT03581240 | Wake Forest University Health Sciences|K C Pharmaceuticals Inc. |
Neuroblastoma|Medulloblastoma|Typical Teratoid Rhabdoid Tumor|Embryonal Tumor With Abundant Neuropil and True Rosettes|Ependymoblastoma|Medulloepithelioma
|
||
| NCT04301843 | Wake Forest University Health Sciences|K C Pharmaceuticals Inc.|Beat NB Cancer Foundation|Team Parker for Life |
Neuroblastoma
|
September 25, 2020 | Phase 2 |
| NCT00176995 | Hordinsky, Maria K., MD|University of Minnesota |
Pseudofolliculitis Barbae
|
March 1999 | Phase 2 |
| NCT03794349 | Children´s Oncology Group|National Cancer Institute (NCI) |
High Risk Neuroblastoma|Recurrent Neuroblastoma|Refractory Neuroblastoma
|
May 28, 2019 | Phase 2 |
| NCT00006079 | M.D. Anderson Cancer Center|National Cancer Institute (NCI) |
Cervical Cancer|Precancerous Condition
|
June 19, 1998 | Phase 2 |
| NCT01483144 | Cancer Prevention Pharmaceuticals, Inc. |
Familial Adenomatous Polyposis
|
October 2013 | Phase 3 |
| NCT00118365 | National Cancer Institute (NCI) |
Precancerous Condition
|
July 1998 | Phase 3 |
| NCT00005884 | University of Wisconsin, Madison|National Cancer Institute (NCI) |
Non-melanomatous Skin Cancer
|
Phase 3 | |
| NCT00086736 | University of Alabama at Birmingham|National Cancer Institute (NCI) |
Prostate Cancer
|
November 2001 | Phase 2 |
| NCT01245816 | Cancer Prevention Pharmaceuticals, Inc. |
Familial Adenomatous Polyposis
|
March 2011 | Phase 3 |
| NCT00003814 | National Cancer Institute (NCI) |
Bladder Cancer
|
February 1999 | Phase 3 |
| NCT00489658 | Epicentre|Médecins Sans Frontières, France |
Trypanosomiasis, African
|
October 2002 | Phase 2|Phase 3 |
| NCT02030964 | New Approaches to Neuroblastoma Therapy Consortium|National Cancer Institute (NCI) |
Neuroblastoma
|
December 2013 | Phase 1 |
| NCT02679144 | Wake Forest University Health Sciences|Beat NB Cancer Foundation|Team Parker for Life |
Neuroblastoma
|
February 2016 | Phase 2 |
| NCT01059071 | Wake Forest University Health Sciences|Cancer Prevention Pharmaceuticals, Inc.|University of Arizona|University of Hawaii |
Neuroblastoma
|
February 2010 | Phase 1 |
| NCT02139397 | Wake Forest University Health Sciences|Beat NB Cancer Foundation|Because of Ezra|K C Pharmaceuticals Inc. |
Neuroblastoma Recurrent
|
May 2014 | Phase 1|Phase 2 |
| NCT00601640 | University of Arizona|National Cancer Institute (NCI) |
Other Benign Neoplasm of Skin, Unspecified
|
January 2007 | Phase 2 |
| NCT00983580 | National Cancer Institute (NCI) |
Adenomatous Polyp
|
August 20, 2009 | Phase 2 |
| NCT01349881 | SWOG Cancer Research Network|National Cancer Institute (NCI)|Cancer Prevention Pharmaceuticals, Inc. |
Colorectal Neoplasms
|
March 1, 2013 | Phase 3 |
| NCT02395666 | Wake Forest University Health Sciences|Beat NB Cancer Foundation|Because of Ezra|K C Pharmaceuticals Inc. |
Neuroblastoma
|
March 5, 2015 | Phase 2 |
| NCT00330148 | Epicentre|Médecins Sans Frontières, France|Embassy of France in Uganda|National Sleeping Sickness Control Program, Uganda |
Trypanosomiasis, African
|
March 2001 | Phase 3 |
| NCT01817894 | Bispebjerg Hospital |
Hirsutism
|
January 2012 | Phase 4 |
| NCT04403282 | Walter Reed National Military Medical Center |
Pseudofolliculitis Barbae
|
July 2020 | Phase 4 |
| NCT00146627 | Drugs for Neglected Diseases|Medecins Sans Frontieres, Netherlands|PNLTHA-DRC;|PNLTHA-RoC|Epicentre|Swiss Tropical & Public Health Institute|World Health Organization |
Trypanosomiasis, African
|
Phase 3 | |
| NCT05879367 | Orbus Therapeutics, Inc. |
Glioblastoma, IDH-wildtype|Glioblastoma|Glioblastoma Multiforme|Glioblastoma IDH (Isocitrate Dehydrogenase) Wildtype|GBM
|
May 26, 2023 | Phase 1 |
| NCT00021294 | University of Arizona|National Cancer Institute (NCI) |
Non-melanomatous Skin Cancer|Precancerous+Nonmalignant Condition
|
May 2001 | Phase 2 |
| NCT05717153 | Mayo Clinic|National Cancer Institute (NCI) |
Diffuse Glioma|Malignant Glioma
|
March 1, 2023 | Early Phase 1 |
| NCT01685827 | Drugs for Neglected Diseases |
Human African Trypanosomiasis (HAT)|Sleeping Sickness
|
October 2012 | Phase 2|Phase 3 |
| NCT02796261 | Orbus Therapeutics, Inc. |
Anaplastic Astrocytoma|Recurrent Anaplastic Astrocytoma
|
July 2016 | Phase 3 |
| NCT00033371 | National Cancer Institute (NCI) |
Colorectal Cancer|Familial Adenomatous Polyposis
|
December 13, 2001 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 83.33 mg/mL ( 457.43 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 5.4894 mL | 27.4469 mL | 54.8938 mL |
| 5 mM | 1.0979 mL | 5.4894 mL | 10.9788 mL |
| 10 mM | 0.5489 mL | 2.7447 mL | 5.4894 mL |
References
- [1] Burri C, et al. Eflornithine for the treatment of human African trypanosomiasis. Parasitol Res. 2003 Jun;90 Supp 1:S49-52.
- [2] Balfour JA, et al. Topical eflornithine. Am J Clin Dermatol. 2001;2(3):197-201; discussion 202.
- [3] Kumar A, et al. A method to improve the efficacy of topical eflornithine hydrochloride cream. Drug Deliv. 2016 Jun;23(5):1495-501.
- [4] Lipke DW, et al. Eflornithine alters changes in vascular responsiveness associated with coarctation hypertension. Clin Exp Hypertens. 1997 Apr;19(3):297-312.