minoxidil
Trade name: loniten
Approved
Oct 18, 1979
Minoxidil is an orally effective direct acting peripheral vasodilator that reduces elevated systolic and diastolic blood pressure by decreasing peripheral vascular resistance. Minoxidil is also used topically to treat androgenetic alopecia. Microcirculatory blood flow in animals is enhanced or maintained in all systemic vascular beds. In man, forearm and renal vascular resistance decline; forearm blood flow increases while renal blood flow and glomerular filtration rate are preserved. The predominant site of minoxidil action is arterial. Venodilation does not occur with minoxidil; thus, postural hypotension is unusual with its administration. The antihypertensive activity of minoxidil is due to its sulphate metabolite, minoxidil sulfate. Minoxidil is thought to promote the survival of human dermal papillary cells (DPCs) or hair cells by activating both extracellular signal-regulated kinase (ERK) and Akt and by preventing cell death by increasing the ratio of BCl-2/Bax. Minoxidil may stimulate the growth of human hairs by prolonging anagen through these proliferative and anti-apoptotic effects on DPCs. Minoxidil, when used as a vasodilator, acts by opening adenosine triphosphate-sensitive potassium channels in vascular smooth muscle cells. This vasodilation may also improve the viability of hair cells or hair follicles. Minoxidil is used for the treatment of severe hypertension and in the topical treatment (regrowth) of androgenic alopecia in males and females and stabilisation of hair loss in patients with androgenic alopecia. — NCATS
Clinical trial activity
84 trials · 89 clinical orgs · 28 marketing orgs
Earliest trial started Oct 1, 2003 (NCT00151515)
Timeline
1970s
- Oct 18, 1979
Earliest FDA Approval
- Oct 18, 1979
Pharmacia & Upjohn — NDA Secondary Org
- Oct 18, 1979
Pfizer — Marketing Organization
- Oct 18, 1979
Pfizer — NDA Secondary Org
1980s
- Mar 3, 1987
Watson Pharmaceuticals — Marketing Organization
- Jul 15, 1988
Quantum Pharmaceutical — Marketing Organization
- Aug 17, 1988
Johnson and Johnson — NDA Secondary Org
- Nov 14, 1988
Par Pharmaceuticals — Marketing Organization
- Nov 14, 1988
Endo Pharmaceuticals — Marketing Organization
1990s
- Dec 13, 1995
Sun Pharmaceuticals — Marketing Organization
- Dec 14, 1995
Mutual Pharmaceutical — Marketing Organization
- Apr 5, 1996
P&L Development — Marketing Organization
- Apr 5, 1996
Actavis — Marketing Organization
- Apr 5, 1996
Teva — Marketing Organization
- Apr 9, 1996
Bausch & Lomb — Marketing Organization
- May 23, 1996
Copley Pharmaceuticals — Marketing Organization
- Oct 18, 1996
Sight Pharms — Marketing Organization
- Dec 24, 1996
Hi Tech Pharmaceuticals — Marketing Organization
- Dec 24, 1996
Akorn, Inc. — Marketing Organization
- Dec 24, 1996
Hikma — Marketing Organization
- Feb 28, 1997
Wockhardt — Marketing Organization
- Feb 28, 1997
Aurobindo Pharma — Marketing Organization
- Apr 29, 1998
Apotex — Marketing Organization
- Jul 30, 1999
Perrigo — Marketing Organization
2000s
- Nov 17, 2000
Avacor Prods — Marketing Organization
- Jan 1, 2003
Johnson and Johnson — Earliest Phase 3 Sponsor(trial)
- Aug 24, 2004
Ei Inc — Marketing Organization
- Aug 24, 2004
PURE SOURCE — Marketing Organization
- Jan 1, 2005
Earliest Phase 2 Sponsor(trial)
2010s
- Jan 1, 2012
Earliest Phase 1 Sponsor(trial)
- Dec 31, 2018
Taro Pharmaceuticals — Marketing Organization
Indications
Studied for
- Acne Vulgaris · Phase 1/Phase 2
- Alopecia · Phase 4
- Alopecia Areata · Phase 4
- Breast Neoplasms · Early Phase 1
- Cancer Survivors · Phase 2
- Dermatology · Phase 1/Phase 2
- Drug-Related Side Effects and Adverse Reactions · Phase 1/Phase 2
- Eye Diseases, Hereditary · Phase 4
- Hair · Phase 4
- Hair Color · Phase 4
- Healthy Volunteers · Phase 1
- Hypotrichosis · Phase 4
- Ludwig's Angina · Phase 2
- Ovarian Neoplasms · Phase 2
- Pharmacokinetics · Phase 1
- Polycystic Kidney Diseases · Phase 3
- Self-Assessment · Phase 1/Phase 2
- Williams Syndrome · Phase 2
Mechanism of action
Sulfonylurea receptor 2, Kir6.2 opener
SUR2 is binding site
Approval history
- approvedPriority reviewOct 18, 1979
Chemistry & pharmacology
SMILES
NC1=NC(=CC(N)=[N+]1[O-])N2CCCCC2- Mol. weight
- 209.2483 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral, Topical
- Availability
- Over the Counter
Oral
Yes
Parenteral
No
Topical
Yes
Sources
- WikipediaMinoxidil ↗
- NCATS5965120SH1 ↗
- ChEMBLCHEMBL802 ↗
Also known as
- 2,4-diamino-6-piperidinopyrimidine 3-oxide
- 2,4-diamino-6-piperidinopyrimidine 3-oxide
- 6-piperidin-1-ylpyrimidine-2,4-diamine 3-oxide
- 6-piperidin-1-ylpyrimidine-2,4-diamine 3-oxide
- alostil
- alostil
- apo-gain
- apo-gain
- loniten
- loniten
- loniten
- loniten
- lonolox
- lonolox
- lonolox
- men's rogaine
- men's rogaine
- minodyl
- minodyl
- minossidile
- minossidile
- minoxidil
- minoxidil
- minoxidil
- minoxidil
- minoxidil
- minoxidil
- minoxidil
- minoxidil
- minoxidil
- minoxidil
- minoxidil
- minoxidil extra strength
- minoxidilum
- minoxidilum
- minoximen
- minoximen
- normoxidil
- normoxidil
- regaine
- regaine
- regaine for men
- regaine for women
- rogaine
- rogaine
- rogaine
- rogaine extra strength
- sm04554
- theroxidil
- theroxidil
- tricoxidil
- tricoxidil
- u-10858
- u-10858
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07264790 | Phase 1 | Dec 31, 2025 | Duke University |
| NCT07273799 | Phase 3 | Dec 20, 2025 | Sheikh Zayed Medical College |
| NCT07203599 | Phase 1/Phase 2 (Phase 2) | Sep 20, 2025 | Shenzhen University |
| NCT06924632 | Phase 3 | Jul 14, 2025 | Samson Clinical Operations Pty Ltd |
| NCT07056933 | N/A | Jul 8, 2025 | Cairo University |
| NCT07012486 | Early Phase 1 (Phase 1) | Jun 30, 2025 | Fudan University |
| NCT07018349 | N/A | Jun 15, 2025 | Jinnah Postgraduate Medical Centre |
| NCT07011485 | Phase 2 | May 14, 2025 | PDFE Pharma Innovations FZCO |
| NCT06826001 | Phase 2 | Feb 28, 2025 | Sheikh Zayed Medical College |
| NCT07080931 | Phase 3 | Feb 24, 2025 | Sunshine Lake Pharma Co., Ltd. |
| NCT06813963 | Phase 4 | Feb 15, 2025 | Southern Medical University |
| NCT06501924 | Phase 3 | Jan 15, 2025 | Applied Biology, Inc., Daniel Alain, Inc., Follea International Limited, University of Roma La Sapienza |
| NCT07076706 | Phase 2 | Dec 5, 2024 | Government of China, Peking University |
| NCT06679556 | Phase 1 | Nov 6, 2024 | Samson Clinical Operations Pty Ltd |
| NCT06590779 | N/A | Nov 2, 2024 | Cosmetique Active International, University of Nice Sophia Antipolis, University of Paris |
| NCT06484881 | Phase 3 | Sep 15, 2024 | Applied Biology, Inc., Follea International Limited, University of Roma La Sapienza |
| NCT06556056 | N/A | Jun 30, 2024 | NovoBliss Research Pvt Ltd |
| NCT05888922 | Phase 3 | Mar 31, 2024 | BioClever 2005 S.L., Bioskin GmbH, Industrial Farmaceutica Cantabria, Spain |
| NCT07038941 | Phase 1 | Mar 19, 2024 | Government of China, Peking University |
| NCT06015516 | Phase 1 | Feb 29, 2024 | Industrial Farmaceutica Cantabria, Spain |
Organizations
Research & Development (89)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Mae Fah Luang University Hospital | Academic/Hospital | 5 | 5 | 2 | 2011 |
| University of Indonesia | Academic/Hospital | 5 | 5 | 3 | 2021 |
| Johnson and Johnson | For profit | 4 | 3 | 2 | 2003 |
| Applied Biology, Inc. | For profit | 3 | 3 | 2 | 2016 |
| Assiut University | Academic/Hospital | 3 | 3 | 3 | 2020 |
| Biosplice Therapeutics | For profit | 3 | 3 | 2 | 2014 |
| Cairo University | Academic/Hospital | 3 | 3 | 3 | 2016 |
| University of Roma La Sapienza | Academic/Hospital | 3 | 0 | 2 | 2016 |
| Allergan | For profit | 2 | 2 | 1 | 2011 |
| Aneira Pharma, Inc. | For profit | 2 | 2 | 1 | 2023 |
| Follea International Limited | For profit | 2 | 0 | 1 | 2024 |
| Galderma | For profit | 2 | 2 | 1 | 2015 |
| Government of China | Government | 2 | 2 | 2 | 2024 |
| Humboldt University | Academic/Hospital | 2 | 2 | 2 | 2008 |
| Industrial Farmaceutica Cantabria, Spain | For profit | 2 | 2 | 2 | 2024 |
| Mayo Clinic | Academic/Hospital | 2 | 1 | 2 | 2006 |
| MFL University Hospital, Bangkok | Academic/Hospital | 2 | 0 | 1 | 2012 |
| Peking University | Academic/Hospital | 2 | 0 | 2 | 2024 |
| PT. Kimia Farma (Persero) Tbk | For profit | 2 | 0 | 2 | 2021 |
| Samson Clinical Operations Pty Ltd | For profit | 2 | 2 | 2 | 2024 |
Marketing (36)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Actavis | For profit | MKTG | Apr 5, 1996 |
| Akorn, Inc. | For profit | MKTG | Dec 24, 1996 |
| Apotex | For profit | MKTG | Apr 29, 1998 |
| Aurobindo Pharma | For profit | SYN | Apr 22, 2024 |
| Aurobindo Pharma | For profit | MKTG | Feb 28, 1997 |
| Avacor Prods | For profit | MKTG | Nov 17, 2000 |
| Bausch & Lomb | For profit | MKTG | Apr 9, 1996 |
| Copley Pharmaceuticals | For profit | MKTG | May 23, 1996 |
| Ei Inc | For profit | MKTG | Aug 24, 2004 |
| Endo Pharmaceuticals | For profit | MKTG | Nov 14, 1988 |
| Hi Tech Pharmaceuticals | For profit | MKTG | Dec 24, 1996 |
| Hikma | For profit | MKTG | Dec 24, 1996 |
| Johnson and Johnson | For profit | NDA2 | Aug 17, 1988 |
| Mutual Pharmaceutical | For profit | MKTG | Dec 14, 1995 |
| P&L Development | For profit | MKTG | Apr 5, 1996 |
| PURE SOURCE | For profit | MKTG | Aug 24, 2004 |
| Par Pharmaceuticals | For profit | MKTG | Nov 14, 1988 |
| Perrigo | For profit | MKTG | Jul 30, 1999 |
| Perrigo | For profit | SYN | Jun 13, 2001 |
| Perrigo | For profit | SYN | Apr 28, 2011 |
| Perrigo | For profit | SYN | Mar 15, 2002 |
| Perrigo | For profit | SYN | Apr 28, 2011 |
| Pfizer | For profit | MKTG | Oct 18, 1979 |
| Pfizer | For profit | NDA2 | Oct 18, 1979 |
| Pharmacia & Upjohn | For profit | NDA2 | Oct 18, 1979 |
| Quantum Pharmaceutical | For profit | MKTG | Jul 15, 1988 |
| Sight Pharms | For profit | MKTG | Oct 18, 1996 |
| Sun Pharmaceuticals | For profit | MKTG | Dec 13, 1995 |
| Taro Pharmaceuticals | For profit | SYN | Dec 31, 2018 |
| Taro Pharmaceuticals | For profit | MKTG | Dec 31, 2018 |
| Teva | For profit | MKTG | Apr 5, 1996 |
| Upjohn | For profit | NDA | — |
| Upsher-Smith Laboratories | For profit | MKTG | — |
| Watson Pharmaceuticals | For profit | MKTG | Mar 3, 1987 |
| Watson Pharmaceuticals | For profit | SYN | Feb 17, 2017 |
| Wockhardt | For profit | MKTG | Feb 28, 1997 |