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DRUG CLASS:

Tyrosinase inhibitor

6ms
Trial completion date
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BRAF (B-raf proto-oncogene)
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BRAF mutation • BRAF V600
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Libtayo (cemiplimab-rwlc) • BNT111
11ms
Bee pollen peptides as potent tyrosinase inhibitors with anti-melanogenesis effects in murine b16f10 melanoma cells and zebrafish embryos. (PubMed, Sci Rep)
Melanin synthesis suppression was examined via qRT-PCR, and western blot in MITF, TYR, TRP-1, and TRP-2. Cell death in zebrafish embryos was evaluated in vivo using a toxicity assay which revealed no significant influence from VY-9, while anti-melanogenic effects were observed when the concentration was 4 µM, suggesting bee pollen-derived peptides' potential in cosmetic and pharmaceutical depigmentation applications.
Preclinical • Journal
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MITF (Melanocyte Inducing Transcription Factor)
over1year
Trial primary completion date
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BRAF (B-raf proto-oncogene)
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Libtayo (cemiplimab-rwlc) • BNT111
over1year
Expression of the tumor antigens NY-ESO-1, tyrosinase, MAGE-A3, and TPTE in pediatric and adult melanoma: a retrospective case control study. (PubMed, Virchows Arch)
BNT111, an investigational lipoplex-formulated mRNA-based therapeutic cancer vaccine encoding melanoma TAAs NY-ESO-1, tyrosinase, MAGE-A3, and TPTE, is undergoing clinical testing in adults. All four TAAs were expressed in pediatric melanoma, albeit NY-ESO-1 and MAGE-A3 to a lesser extent than in adult melanoma. These data support the possibility of investigating vaccines targeting these TAAs for the treatment of pediatric melanoma.
Retrospective data • Journal • IO biomarker
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CTAG1B (Cancer/testis antigen 1B)
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BNT111
2years
Enrollment closed
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BRAF (B-raf proto-oncogene)
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BRAF mutation • BRAF V600
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Libtayo (cemiplimab-rwlc) • BNT111
over2years
Trial With BNT111 and Cemiplimab in Combination or as Single Agents in Patients With Anti-PD-1-refractory/Relapsed, Unresectable Stage III or IV Melanoma (clinicaltrials.gov)
P2, N=180, Recruiting, BioNTech SE | Trial completion date: Jun 2025 --> Jul 2026 | Trial primary completion date: Oct 2024 --> Nov 2025
Trial completion date • Trial primary completion date
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BRAF (B-raf proto-oncogene)
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BRAF mutation • BRAF V600
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Libtayo (cemiplimab-rwlc) • BNT111
over2years
Trial completion • Metastases
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CTAG1B (Cancer/testis antigen 1B)
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BNT111
over2years
Discovery of amphotericin B, an antifungal drug as tyrosinase inhibitor with potent anti-melanogenic activity. (PubMed, Int J Biol Macromol)
Although hydroquinone, kojic acid, and arbutin are the most well-known tyrosinase inhibitors, their adverse effects are inevitable...Mechanistically, amphotericin B treatment significantly activated ERK and Akt signaling pathways, resulting in the decreased expression of MITF and tyrosinase. The obtained results may pursue pre-clinical and clinical studies to examine the possibility of using amphotericin B as an alternative treatment for hyperpigmentation disorders.
Journal
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MITF (Melanocyte Inducing Transcription Factor)
over2years
Homobimetallic Au(I)-Au(I) and Heterotrimetallic Au(I)-Fe(II)-Au(I) Complexes with Dialkyldithiophosphates and Phosphine Ligands: Structural Characterization, DFT Analysis, and Tyrosinase Inhibitory and Biological Effects. (PubMed, ACS Omega)
To investigate the possible cytotoxicities of 2, 3, and 7, in vitro cellular tests were carried out on the human cancerous breast cell line MCF-7. 2 and 7 show promising cytotoxicity.
Journal
over2years
Tripeptides conjugated with thiosemicarbazones: new inhibitors of tyrosinase for cosmeceutical use. (PubMed, J Enzyme Inhib Med Chem)
Mushroom tyrosinase was inhibited by TSC1-conjugates at micromolar level, with IC lower than this for kojic acid, a widely used reference compound. Up to now, this is the first report regarding thiosemicarbazones conjugated with tripeptides, synthesised for the purpose of tyrosinase inhibition.
Journal
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TSC1 (TSC complex subunit 1)
almost3years
Ethyl Gallate Isolated from Castanopsis cuspidata var. sieboldii Branches Inhibits Melanogenesis and Promotes Autophagy in B16F10 Cells. (PubMed, Antioxidants (Basel))
In addition, EG downregulated melanogenetic gene expression and activated autophagy signals. Therefore, EG extracted from CCS branches could serve as a novel functional cosmetic material with antimelanogenic and autophagy-enhancing activity.
Journal
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MITF (Melanocyte Inducing Transcription Factor)
almost3years
Upregulation of CD86 and IL-12 by rhododendrol in THP-1 cells cocultured with melanocytes through ROS and ATP. (PubMed, J Dermatol Sci)
RD is a pro-hapten sensitizer dependent on tyrosinase that induces ROS generation and ATP release from melanocytes for CD86 and IL-12 upregulation in DCs, possibly leading to the generation of tyrosinase-specific cytotoxic T lymphocytes. The coculture system h-CLATw/M may be useful for predicting the sensitizing potential to induce leukoderma.
Journal
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CD86 (CD86 Molecule)