Prof Firas Al-Niaimi is a globally renowned consultant dermatologist, recognised as a leading authority in Mohs surgery and laser treatments, boasting an impressive career spanning nearly two decades. He trained in some of the UK's top hospitals and fellowship-trained in dermatologic surgery and lasers at St. Thomas’ hospital in London where he continued to work as an honorary consultant for several years before moving to fulltime private practice.

At the recent Dermatology Congress held in Cape Town, UK-based dermatologist Prof Firas Al-Niaimi presented on challenges in hyperpigmentation: diagnosis and treatment. The following is based on his presentation.

Prof Al-Niaimi began by stating that skin of colour is going to be a key focus globally in the field of dermatology. He explained that the world is changing, due to various reasons including climate change, and pigmentation is a problem – even in western Europe.

Melanogenesis is a complex process involving melanocyte activation, melanin synthesis, melanin transfer to keratinocytes and melanin embedded in keratinocytes. Tyrosinase inhibition is the most effective and safe solution as it tackles pigmentation at its source.

Lasers aren’t always the answer in pigmentation and topical therapy remains the first-line choice in many types of pigmentation. If active melanogenesis is stable, it will respond to laser therapy. If melanogenesis is unstable, as is the case with melasma, post-inflammatory hyperpigmentation and photodamage, their effects can be unpredictable and, in some cases, can worsen the pigmentation.

In terms of topical melanin synthesis inhibition, hydroquinone-based therapy used to be all that was available to us. This is not suitable to use long term, as it leads to melanocyte toxicity and irritation and hyperpigmentation is a chronic, recurrent condition. This product is not recommended in pregnancy and needs a prescription.

Non-prescription options are cosmeceuticals, including Thiamidol, the first inhibitor designed for human tyrosinase effectively reduces hyperpigmentation. Thiamidol is the best inhibitor of human tyrosinase out of 50 000 compounds tested. Over 1 000 subjects have been enrolled in studies with Thiamidol. It was tested on all prototypes and found to be effective against age spots, facial hyperpigmentation and post-inflammatory hyperpigmentation. The studies revealed that Thiamidol reduces visible light induced pigmentation and no melanocyte toxicity has been observed.

Mechanism of action

Most lightening agents target the key enzyme of melanin synthesis, tyrosinase. However, they were identified using mushroom tyrosinase. “Thiamidol is the first human-derived tyrosinase. It is the most potent inhibitor of human tyrosinase – even in low concentrations, it is highly selective against tyrosinase receptors, and is non-irritant,” Prof Al-Niaimi stated.

Many studies about the human tyrosinase molecule. In a six-month efficacy study, it showed significant decrease of Melasma Area and Severity Index (MASI) scores and more than 50% improvement of MASI scores still visible three months after study end.

Conditions where melanin inhibition is essential

Conditions where melanin inhibition is essential include melasma, post-inflammatory hyperpigmentation, lichen planus pigmentosa, photodamage, and ashy dermatosis. Conditions that require laser treatment are naevus of Ota, cafe au lait macule, acquired bilateral nevus of ota-like macules, maturational hyperpigmentation, nervous zygomaticus, Becker’s naevus.

Thiamidol and lasers

Prof Al-Niaimi explained that no lasers can inhibit melanin synthesis. Topical treatments are almost always needed as an adjunct in unstable or active melanogenesis conditions. Pre-treatment with Thiamidol decreases risk of post-inflammatory hyperpigmentation in high-risk patients. There is a synergistic effect when these two therapies are combined and there is a better response when used as pre-treatment, compared to post treatment. This also reduces the risk of ‘rebound’ and post-inflammatory hyperpigmentation from laser. Pre-treatment with Thiamidol prevents pigmentation development. There was significantly less hyperpigmentation when antipigment dual serum was used three weeks prior to UVB stress.

Dexpanthenol

Dexpanthenol improves skin barrier function, regeneration and natural protection. It moisturises the stratum corneum and reduces transepidemal water loss. It optimises and accelerates wound healing and maintains skins resilience.

A focus on acne

There are four pathogenic factors of acne being excessive production of sebum, abnormal cell turnover, C. acnes colonisation, and inflammation and host immune reaction. Treatment should target as many pathogenic factors as possible.

Researchers biopsied clinically normal follicles from uninvolved skin of acne patients and compared this to lesions from acne patients and healthy controls. The outcome was that elevated levels of markers for inflammation could be found in the follicles of the uninvolved skin of acne patients, comparable to the levels found in lesioned skin. Inflammation is present at all stages of acne ranging from subclinical micro inflammation to inflamed papules or pustules. Subclinical microcomodones are the initial acne lesions that mature into clinically apparent comedones and inflammatory lesions.

Acne is primarily an inflammatory disease, micro inflammation being the root cause of the acne cycle.Adherence is a major limitation in acne treatment, and topical antimicrobial acne treatment tolerability is a significant factor affecting treatment adherence. Compliance to topical acne therapy is generally poor. Side effects are a main reason being dryness, redness and irritation.

Acne leads to inflammation being intra inflammatory hyperpigmentation and then post inflammatory hyperpigmentation. So there is always a degree of inflammation, which varies, and there is always microinflammation. This is why patients get post-inflammatory hyperpigmentation. Post-inflammatory hyperpigmentation can take up to five years to settle. “It is important to control this as well as the acne. Isotretinoin won’t address post-inflammatory hyperpigmentation,” Prof Al-Niaimi said. Any treatment must consider UV protection including blue high energy visible light as visible light plays a role in melasma and post inflammatory hyperpigmentation in darker skin types.

Licochalcone A is an anti-inflammatory ingredient, which calms skin irritation and visibly reduces redness. It reduces many inflammatory mediators, reducing pro-inflammatory cytokines, inhibiting eicosanoid production and inhibiting AP-1.

Conclusion

Prof Al-Niaimi emphasised that Thiamidol is the first human tyrosinase inhibitor effective in reducing hyperpigmentation with no melanocyte toxicity. There is strong clinical evidence behind the molecule and it is an effective cosmeceutical treatment for hyperpigmentation for all skin types and all skin tones.

Thamidol is patented molecule by Eucerin.