- An agent previously in clinical development as a topical anti-inflammatory is retargeted for hyperpigmentation using nPharmakon’s computational technology
- First-in-class topically bioavailable selective KIT kinase inhibitor with anti-inflammatory activity (COX / 5-Lipoxygenase inhibitor)
- Statistically significant superiority to vehicle and commercial comparator is seen in both visual scoring and instrumentally measured L*a*b* L values
PISCATAWAY, NJ, USA I July 1, 2015 I nPharmakon LLC, a life sciences company focused on “retargeting” — the identification of previously unrecognized molecular targets of clinically tested therapeutic agents and their subsequent development for new uses — announced today the results from a clinical study of NPH29, the company’s development candidate for skin hyperpigmentation. In a double-blind, within-subject, nurse-administered 30 day study involving 21 study participants, NPH29 1% cream has demonstrated statistically significant superiority to vehicle cream and the commercial comparator, a best-selling product in Japan with tranexamic acid as the active ingredient, in both visual scoring and instrumentally measured L*a*b* L values (p < 0.005); no adverse events attributable to the NPH29 cream were observed.
“This is a major milestone for our company,” said Dr. Felix Sheinerman, Chief Scientific Officer of nPharmakon. “The NPH29 story demonstrates the potential of the company’s retargeting approach to quickly advance “de-risked” assets from computational predictions to demonstration of activity in pre-clinical models to clinical proof of concept in new indications.”
“There is a great need for safe and efficacious treatments for skin hyperpigmentation conditions with a mechanism of action other than tyrosinase inhibition,” said Dr. Dmitri Rebatchouk, CEO of nPharmakon. “Given the prior clinical history of NPH29 and the new data demonstrating its efficacy in reducing pigmentation, we believe NPH29 can now be rapidly developed and launched as a new treatment for various hyperpigmentation disorders, providing a new option to patients — articularly to those for whom other treatments have not been effective. Since NPH29 is both a KIT inhibitor and an anti-inflammatory, it could prove to be particularly useful for treatment of peri-inflammatory and post-inflammatory hyperpigmentation, such as hyperpigmentation accompanying acne.”
About skin hyperpigmentation disorders
Skin hyperpigmentation is highly prevalent worldwide, notably in Asia, and in individuals with medium to dark skin tone (Fitzpatrick skin type III to V); skin blemishes of localized hyperpigmentation can be highly distressing and have a material negative impact on the quality of life of the sufferers. Examples of skin hyperpigmentation disorders include post-inflammatory hyperpigmentation, e.g. pigmentation following acne and other inflammatory skin disorders; melasma; and pigmentation following medical and cosmetic procedures. Only products containing hydroquinone are approved by the US FDA for the treatment of hyperpigmentation. Hydroquinone, developed in the 1950s, is restricted or banned in Europe and in many Asian countries due to irritancy and other safety concerns. New effective and safe treatments are greatly needed.
About KIT inhibition as a therapeutic strategy for skin hyperpigmentation
KIT ligand (also called Stem Cell Factor, or SCF) – KIT receptor tyrosine kinase signaling pathway is a master regulator of skin and hair pigmentation, and KIT inhibition is a validated strategy for reduction of skin pigmentation. KIT kinase is expressed in skin and hair follicle melanocytes (the cell type responsible for skin pigmentation) and controls expression of enzymes that make the skin pigment melanin. KIT and KIT ligand are overexpressed in melasma, a common skin hyperpigmentation disorder. Up-regulation of KIT signaling by injection of KIT ligand or by a KIT ligand gain-of-function genetic mutation increases pigmentation, whereas down-regulation of KIT signaling reduces pigmentation. Further, reversible reduction of skin pigmentation is reported in ~70% of cancer patients taking systemic KIT inhibitor drugs.
About NPH29
NPH29 (nPharmakon development code) was under development in the early 1990s as a topical anti-inflammatory and advanced to Phase III clinical studies. nPharmakon discovered that in addition to its previously known activity against COX enzymes and 5-lipoxygenase, NPH29 potently and selectively inhibits KIT kinase and is potentially useful for treatment of skin hyperpigmentation. An nPharmakon patent covering the use of NPH29 for hyperpigmentation disorders and skin lightening was issued in Japan in 2014; the company has received a Notice of Allowance in the USA in June 2015. PCT patent applications are in prosecution in Europe, P.R. China, Taiwan, S. Korea and other jurisdictions.
About nPharmakon LLC
nPharmakon LLC is a privately held drug discovery and development company focused on the identification of new therapeutic opportunities for clinically tested investigational and approved drugs. The company’s proprietary computational chemogenomics technology is based on rapid, accurate analysis of similarities between drugs and tool compounds reported in literature and patents as potent modulators of various protein targets. For more information, please visit the company’s website at www.npharmakon.com
SOURCE: nPharmakon
Post Views: 35
- An agent previously in clinical development as a topical anti-inflammatory is retargeted for hyperpigmentation using nPharmakon’s computational technology
- First-in-class topically bioavailable selective KIT kinase inhibitor with anti-inflammatory activity (COX / 5-Lipoxygenase inhibitor)
- Statistically significant superiority to vehicle and commercial comparator is seen in both visual scoring and instrumentally measured L*a*b* L values
PISCATAWAY, NJ, USA I July 1, 2015 I nPharmakon LLC, a life sciences company focused on “retargeting” — the identification of previously unrecognized molecular targets of clinically tested therapeutic agents and their subsequent development for new uses — announced today the results from a clinical study of NPH29, the company’s development candidate for skin hyperpigmentation. In a double-blind, within-subject, nurse-administered 30 day study involving 21 study participants, NPH29 1% cream has demonstrated statistically significant superiority to vehicle cream and the commercial comparator, a best-selling product in Japan with tranexamic acid as the active ingredient, in both visual scoring and instrumentally measured L*a*b* L values (p < 0.005); no adverse events attributable to the NPH29 cream were observed.
“This is a major milestone for our company,” said Dr. Felix Sheinerman, Chief Scientific Officer of nPharmakon. “The NPH29 story demonstrates the potential of the company’s retargeting approach to quickly advance “de-risked” assets from computational predictions to demonstration of activity in pre-clinical models to clinical proof of concept in new indications.”
“There is a great need for safe and efficacious treatments for skin hyperpigmentation conditions with a mechanism of action other than tyrosinase inhibition,” said Dr. Dmitri Rebatchouk, CEO of nPharmakon. “Given the prior clinical history of NPH29 and the new data demonstrating its efficacy in reducing pigmentation, we believe NPH29 can now be rapidly developed and launched as a new treatment for various hyperpigmentation disorders, providing a new option to patients — articularly to those for whom other treatments have not been effective. Since NPH29 is both a KIT inhibitor and an anti-inflammatory, it could prove to be particularly useful for treatment of peri-inflammatory and post-inflammatory hyperpigmentation, such as hyperpigmentation accompanying acne.”
About skin hyperpigmentation disorders
Skin hyperpigmentation is highly prevalent worldwide, notably in Asia, and in individuals with medium to dark skin tone (Fitzpatrick skin type III to V); skin blemishes of localized hyperpigmentation can be highly distressing and have a material negative impact on the quality of life of the sufferers. Examples of skin hyperpigmentation disorders include post-inflammatory hyperpigmentation, e.g. pigmentation following acne and other inflammatory skin disorders; melasma; and pigmentation following medical and cosmetic procedures. Only products containing hydroquinone are approved by the US FDA for the treatment of hyperpigmentation. Hydroquinone, developed in the 1950s, is restricted or banned in Europe and in many Asian countries due to irritancy and other safety concerns. New effective and safe treatments are greatly needed.
About KIT inhibition as a therapeutic strategy for skin hyperpigmentation
KIT ligand (also called Stem Cell Factor, or SCF) – KIT receptor tyrosine kinase signaling pathway is a master regulator of skin and hair pigmentation, and KIT inhibition is a validated strategy for reduction of skin pigmentation. KIT kinase is expressed in skin and hair follicle melanocytes (the cell type responsible for skin pigmentation) and controls expression of enzymes that make the skin pigment melanin. KIT and KIT ligand are overexpressed in melasma, a common skin hyperpigmentation disorder. Up-regulation of KIT signaling by injection of KIT ligand or by a KIT ligand gain-of-function genetic mutation increases pigmentation, whereas down-regulation of KIT signaling reduces pigmentation. Further, reversible reduction of skin pigmentation is reported in ~70% of cancer patients taking systemic KIT inhibitor drugs.
About NPH29
NPH29 (nPharmakon development code) was under development in the early 1990s as a topical anti-inflammatory and advanced to Phase III clinical studies. nPharmakon discovered that in addition to its previously known activity against COX enzymes and 5-lipoxygenase, NPH29 potently and selectively inhibits KIT kinase and is potentially useful for treatment of skin hyperpigmentation. An nPharmakon patent covering the use of NPH29 for hyperpigmentation disorders and skin lightening was issued in Japan in 2014; the company has received a Notice of Allowance in the USA in June 2015. PCT patent applications are in prosecution in Europe, P.R. China, Taiwan, S. Korea and other jurisdictions.
About nPharmakon LLC
nPharmakon LLC is a privately held drug discovery and development company focused on the identification of new therapeutic opportunities for clinically tested investigational and approved drugs. The company’s proprietary computational chemogenomics technology is based on rapid, accurate analysis of similarities between drugs and tool compounds reported in literature and patents as potent modulators of various protein targets. For more information, please visit the company’s website at www.npharmakon.com
SOURCE: nPharmakon
Post Views: 35
