"Your hair is a statement of style, an affirmation of beauty, and an expression of self-love." - Ademola Mandela
In the context of drug development and medical research, compounds that have demonstrated promise in preclinical investigations and advanced to the point of being evaluated in human subject’s clinical trials are referred to as clinical candidates. Clinical candidates serve a variety of purposes in the field of androgenetic alopecia (AGA)
| ID | COMPOUND NAME | FORMULA | CAS | MECHANISM_OF ACTION | THERAPY | DOSAGE | FDA APPROVAL | MARKETED NAME | ADVERSE EFFECTS | sex | MEDIATIONS | REFERENES |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 1 | Minoxidil | C9H15N5O | 38304-91-5 | Arteriolar vasodilation, inducing cell proliferation; increase vascular endothelial growth factor | Topical | 2–10%; QD, BID | 1988 | Loniten, Minodyl, and Minoxidil HTN | Headaches, hypertrichosis, irritation, contact dermatitis | B | Minoxidil is a medication used for the treatment of high blood pressure and pattern hair loss. It is an antihypertensive vasodilator | Devjani S, Ezemma O, Kelley KJ, Stratton E, Senna M. Androgenetic Alopecia: Therapy Update. Drugs. 2023 Jun;83(8):701-715. doi: 10.1007/s40265-023-01880-x. Epub 2023 May 11. PMID: 37166619; PMCID: PMC10173235 |
| 2 | FinasteridE | C23H36N2O2 | 98319-26-7 | 5-alpha-reductase inhibitor—blocks formation of DHT | Topical | 0.25% spray, 1% gel; QD, BID | 9/9/2003 | Proscar and Propecia | Irritation, erythema, contact dermatitis | M | Finasteride, sold under the brand names Proscar and Propecia among others, is a medication used to treat pattern hair loss and benign prostatic hyperplasia in men. It can also be used to treat excessive hair growth in women | Devjani S, Ezemma O, Kelley KJ, Stratton E, Senna M. Androgenetic Alopecia: Therapy Update. Drugs. 2023 Jun;83(8):701-715. doi: 10.1007/s40265-023-01880-x. Epub 2023 May 11. PMID: 37166619; PMCID: PMC10173235 |
| 3 | Latanoprost | C26H40O5 | 130209-82-4 | Prostaglandin analog—prolong anagen (growth) phase | Topical | 0.1% QD | 1996 | Xalatan and Xelpros | Irritation, hypertrichosis | B | Latanoprost, sold under the brand name Xalatan among others, is a medication used to treat increased pressure inside the eye. This includes ocular hypertension and open angle glaucoma | Devjani S, Ezemma O, Kelley KJ, Stratton E, Senna M. Androgenetic Alopecia: Therapy Update. Drugs. 2023 Jun;83(8):701-715. doi: 10.1007/s40265-023-01880-x. Epub 2023 May 11. PMID: 37166619; PMCID: PMC10173235 |
| 4 | Finasteride | C23H36N2O2 | 98319-26-7 | Type II 5-alpha-reductase inhibitor—blocks formation of DHT | Oral | 1 mg, 5 mg; QD | NA | Proscar and Propecia | Sexual dysfunction, altered libido, gynecomastia, mood changes | M | Finasteride used to treat symptoms of BPH such as frequent and difficult urination and may reduce the chance of acute urinary retention (sudden inability to urinate) | Devjani S, Ezemma O, Kelley KJ, Stratton E, Senna M. Androgenetic Alopecia: Therapy Update. Drugs. 2023 Jun;83(8):701-715. doi: 10.1007/s40265-023-01880-x. Epub 2023 May 11. PMID: 37166619; PMCID: PMC10173235 |
| 5 | Dutasteride | C27H30F6N2O2 | 164656-23-9 | Type I and II 5-alpha-reductase inhibitor—blocks formation of DHT | Oral | 0.5 mg, 1 mg, QD | 11/20/2001 | Avodart | Sexual dysfunction, altered libido, gynecomastia, mood changes | B | Dutasteride, sold under the brand name Avodart among others, is a medication primarily used to treat the symptoms of a benign prostatic hyperplasia, an enlarged prostate not associated with cancer | Devjani S, Ezemma O, Kelley KJ, Stratton E, Senna M. Androgenetic Alopecia: Therapy Update. Drugs. 2023 Jun;83(8):701-715. doi: 10.1007/s40265-023-01880-x. Epub 2023 May 11. PMID: 37166619; PMCID: PMC10173235 |
| 6 | spironolactone | C24H32O4S | 52-01-7 | Antiandrogen—effectively decreases testosterone | Oral | 12–200 mg QD | 8/20/2001 | Aldactone | Postural hypotension, electrolyte imbalances | F | Spironolactone, sold under the brand name Aldactone among others, is a medication that is primarily used to treat fluid build-up due to heart failure, liver scarring, or kidney disease | Devjani S, Ezemma O, Kelley KJ, Stratton E, Senna M. Androgenetic Alopecia: Therapy Update. Drugs. 2023 Jun;83(8):701-715. doi: 10.1007/s40265-023-01880-x. Epub 2023 May 11. PMID: 37166619; PMCID: PMC10173235 |
| 7 | spironolactone | C24H32O4S | 52-01-7 | Antiandrogen—effectively decreases testosterone | Oral | 12–200 mg QD | 8/20/2001 | Aldactone | Postural hypotension, electrolyte imbalances | F | Spironolactone, sold under the brand name Aldactone among others, is a medication that is primarily used to treat fluid build-up due to heart failure, liver scarring, or kidney disease | Devjani S, Ezemma O, Kelley KJ, Stratton E, Senna M. Androgenetic Alopecia: Therapy Update. Drugs. 2023 Jun;83(8):701-715. doi: 10.1007/s40265-023-01880-x. Epub 2023 May 11. PMID: 37166619; PMCID: PMC10173235 |
| 8 | flutamide | C11H11F3N2O3 | 13311-84-7 | Antiandrogen—effectively blocks testosterone | Oral | 62.5–250 mg QD | 6/11/1905 | Eulexin | Elevated liver enzymes, bloating, headache, breast tenderness | F | Flutamide, sold under the brand name Eulexin among others, is a nonsteroidal antiandrogen which is used primarily to treat prostate cancer. It is also used in the treatment of androgen-dependent conditions like acne, excessive hair growth, and high androgen levels in women | Devjani S, Ezemma O, Kelley KJ, Stratton E, Senna M. Androgenetic Alopecia: Therapy Update. Drugs. 2023 Jun;83(8):701-715. doi: 10.1007/s40265-023-01880-x. Epub 2023 May 11. PMID: 37166619; PMCID: PMC10173235 |
| 9 | Bicalutamide | C18H14F4N2O4S | 90357-06-5 | Antiandrogen—effectively blocks testosterone | Oral | 12.5–50 mg 3–5 times weekly | 6/17/1905 | Casodex, Cosudex, Calutide, Calumid, and Kalumid | Elevated liver enzymes, bloating, headache, breast tenderness | F | Bicalutamide, sold under the brand name Casodex among others, is an antiandrogen medication that is primarily used to treat prostate cancer. It is typically used together with a gonadotropin-releasing hormone analogue or surgical removal of the testicles to treat metastatic prostate cancer | Devjani S, Ezemma O, Kelley KJ, Stratton E, Senna M. Androgenetic Alopecia: Therapy Update. Drugs. 2023 Jun;83(8):701-715. doi: 10.1007/s40265-023-01880-x. Epub 2023 May 11. PMID: 37166619; PMCID: PMC10173235 |
| 10 | cyproterone acetate | C22H27ClO3 | 2098-66-0 | Antiandrogen—blocks gonadotropin-releasing hormone and androgen receptors | Oral | 2 mg QD (often combined with ethinyl estradiol) | NA | Androcur, Androcur Depot, Androcur-100, Androstat, Asoteron, Cyprone, Cyproplex, Cyprostat, Cysaxal, Imvel, and Siterone | Weight gain, breast tenderness, decreased libido | B | Cyproterone, also known by its developmental code name SH-80881, is a steroidal antiandrogen which was studied in the 1960s and 1970s but was never introduced for medical use | Devjani S, Ezemma O, Kelley KJ, Stratton E, Senna M. Androgenetic Alopecia: Therapy Update. Drugs. 2023 Jun;83(8):701-715. doi: 10.1007/s40265-023-01880-x. Epub 2023 May 11. PMID: 37166619; PMCID: PMC10173235 |
| 11 | Botulinum toxin A | C6760H10447N1743O2010S32 | 93384-43-1 | Interferes with the suppressive effect of DHT on the hair follicle | Injectables | Injeted every month | 6/7/1905 | Dysport/Azzalure from Galderma and Ipsen, Xeomin/Bocouture from Merz, Jeuveau/Nuceiva from Evolus, manufactured by Daewoong in South Korea | Mild discomfort, temporary drooping of nearby muscles, transient headache, nausea | M | It prevents the release of the neurotransmitter acetylcholine from axon endings at the neuromuscular junction, thus causing flaccid paralysis | https://www.iranjd.ir/article_173914_794b3a1a8216c74e93f88ebd3d059177.pdf |
| 11 | Kopexil | C4H6N4O | 113275-13-1 | Lysyl hydroxylase (LH), an enzyme catalyzes the formation of hydroxylysine, which contributes to the maturation of collagen synthesis | Topical | 2–10%; QD, BID | NA | Aminexil | mild scalp irritations such as redness, itching, and dryness | B | originally used to treat high blood pressure | Mattar MC, Lough D, Pishvaian MJ, Charabaty A. Current management of inflammatory bowel disease and colorectal cancer. Gastrointest Cancer Res. 2011 Mar;4(2):53-61. PMID: 21673876; PMCID: PMC3109885 |
| 12 | Triamcinolone | C21H27FO6 | 124-94-7 | Immunosuppression is the main mechanism of action | By mouth, topical, intranasal, intramuscular, intra-articular, intra-synovial | Concentrations of 2.5 to 10 mg/mL | 6/16/2008 | Kenalog | Burning, itching, irritation, stinging, redness, or drying of the skin. acne. change in skin color. unwanted hair growth | B | Triamcinolone is a glucocorticoid used to treat certain skin diseases, allergies, and rheumatic disorders among others. It is also used to prevent worsening of asthma and COPD | Kumaresan M. Intralesional steroids for alopecia areata. Int J Trichology. 2010 Jan;2(1):63-5. doi: 10.4103/0974-7753.66920. PMID: 21188031; PMCID: PMC3002419 |
| 13 | Baricitinib | C16H17N7O2S | 1187594-09-7 | It acts as an inhibitor of janus kinase, blocking the subtypes JAK1 and JAK2 | Oral | SALT 30response achieved by 29.6%, 33.3%, 17.9% and 10.7% patients treated with baricitinib 2mg, 4mg | 5/31/2018 | Olumiant | Increased cholesterol levels | F | Baricitinib, sold under the brand name Olumiant among others, is an immunomodulatory medication used for the treatment of rheumatoid arthritis, alopecia areata, and COVID-19 | Freitas E, Guttman-Yassky E, Torres T. Baricitinib for the Treatment of Alopecia Areata. Drugs. 2023 Jun;83(9):761-770. doi: 10.1007/s40265-023-01873-w. Epub 2023 May 17. PMID: 37195491; PMCID: PMC10191081 |
| 14 | Ritlecitinib | C22H27N5O4S | 1792180-81-4 | Ritlecitinib is a kinase inhibitor which inhibits Janus kinase 3 and tyrosine kinase | By mouth, topical, intranasal, intramuscular, intra-articular, intra-synovial | 50 mg and 30 mg daily for 24 weeks | Jun-23 | LITFULO | warm, red, or painful skin or sores on your body | B | Ritlecitinib, sold under the brand name Litfulo, is a medication used for the treatment of severe alopecia | Ramírez-Marín HA, Tosti A. Evaluating the Therapeutic Potential of Ritlecitinib for the Treatment of Alopecia Areata. Drug Des Devel Ther. 2022 Feb 17;16:363-374. doi: 10.2147/DDDT.S334727. PMID: 35210753; PMCID: PMC8860347 |
| 15 | biotinoyl tripeptide-1 | C24H38N8O6S | 11534242 | stimulating the extracellular matrix proteins in the hair follicles, promoting cell proliferation, and enhancing the production of hair keratinocytes | Injectables | 1-3% recommend | NA | No known side effects | B | Biotinoyl Tripeptide-1 helps slow the aging effects by lessening harmful dihydrotestosterone (DHT) production, improving irrigation of the hair follicle, stimulating the production of anchoring molecules, and promoting hair growth much as 121% |