Innovative and powerful active

Selectively targets dark sports

Highlights the skin’s natural beauty

Performs better than hydroquinone 2%

TFC-1067

Selectively removes

dark spots

Name : TFC-1067

INCI name : Difluorocyclohexyloxyphenol

Functions: Bleaching - Antioxidants

CAS # 2001566-55-6

Mechanism of action : Human tyrosinase inhibitor

Patent Family : WO2016/139336 (France, Germany, UK, USA, Republic of Korea, China, Japan, Australia, Canada, Mexico, India, Hong Kong)

Lightening Ingredient

Skin lightening

TFC-1067 is a synthetic active, part of the arbutins’ family with no possible break down into hydroquinone

STABILITY AND TRANSCUTANEOUS DIFFUSION

Hydroquinone

Transcutaneous diffusion: with high flux capacity and efficacy, TFC-1067 could be used at very low concentration in simple formulation.

3328

0

20

40

TFC-10670.2%

TFC-10670.01%

Perc

enta

ge

Resorption of TFC-1067

The quantity of TFC-1067 measured in epidermis was higher than that in dermis. TFC-1067 is able to reach the compartment of the skin where its activity is required (on melanocytes).

IN VITRO EFFICACY

TFC-1067 is more effective than deoxyarbutin and alpha-arbutin by inhibiting tyrosinase activity and melanin synthesis in human melanocytes cultures.

0,035

0,272

0,0

0,1

0,2

0,3

TFC-1067 Deoxyarbutin

IC50

(mM

)

8 times greater

Inhibition of Human Tyrosinase Inhibition of Melanin Synthesis by Human Melanocytes in vitro

23

9

16

0

10

20

30

Control TFC-106750 µM

alpha-arbutin300 µM

Mel

anin

synt

hetiz

ed(µ

g/m

l)

Melanin decrease by 61%

Melanin decrease by 29 %

Effect of TFC-1067 over 10 days after a Stimulation by L-tyrosine 1mM (to induce melanin production )

Efficacy on melanoderm skin explants: topical application every 2 days of TFC-1067 at 0.05% decreases melanin content and significantly increases the brightness with no sign of toxicity.

* p<0.05

25

45

65

D0 D7 D11 D14

L(*D

65)

Days

Measure of Brightness

untreated tissuenegative control

TFC-10670.05%

Lightening Effect on MelanodermSkin Explants Over 14 Days

52,7

32,3

0

20

40

60

Untreatedtissue

TFC-1067 0.05%

in acetone:olive oil (4:1)

Mel

anin

cont

ent

(µg)

Melanin decreases

by 40%

No Hydroquinone released - No degradation(tested in the following conditions)

Chemical conditions Biological conditions

Water (ultrapure) 15 DaysBis Tris buffer (pH 6,5) 14 Days

PBS, RT, 14 DaysRinger solutions (pH 6,8), RT 14 DaysRinger solutions (pH 5.5) 70°C, 24hRinger solutions (pH 8,5) 70°C, 24h

Fibroblasts extract, RT, 48hKeratinocyte extract, RT, 48hSkin (tissue extract), RT 48h

Sweat, RT, 48h

Flux determination (Franz cells) on human skin at T24h (n=3)

ng TFC-1067 / g tissue SD (ng/g)

EPIDERMIS 22 278 1 296DERMIS 5 142 831

TFC-1067

TFC-1067 has a free radical scavenging activity (DPPH assay). The antioxidant activity of deoxyarbutin and TFC-1067 are similar and slightly higher than a-arbutin and b-arbutin and closed to Ascorbic Acid 2-Glucoside.TFC-1067 can prevent the damaging effects of the ROS including atypical pigmentation.

100

40

23 2435 31

0

60

120

Trolox AA2G α-Arbutin β-Arbutin deoxyarbutin TFC-1067

Perc

enta

ge

Efficiency factor compared to the reference (Trolox)

Antioxidant Activity

CLINICAL EFFICACY

Face cream treatment TFC-1067 (0.2%) vs Hydroquinone (2%)

Study :

• Face cream containing only one lightening active TFC-1067 (0.2%) or Hydroquinone (2%)

• Skin Lightening Efficacy for 12 weeks. Mean of 23 subjects

Results :

• Dermatologist and subject evaluations• Dermaspectrophotometer readings on dyschromic

(dark spot) or normal skin (assessments for pigmentation on the melanin scale)

TFC-1067 (0.2%) selectively targets dark spots, highlights the skin’s natural beauty and performs better than Hydroquinone (2%).

Using spectrophotometer, a statistically significant improvement was observed on dyschromic skin after 4 to 12 weeks of use. TFC-1067 selectively targets dark spots compared to hydroquinone and leads to a better skin tone uniformization of the dyschromic skin.

A statistically significant improvement was reported : • after 8 weeks of use by the dermatologist and the

subject on the dark spot intensity.• after 12 weeks of use by the dermatologist on both

dark spot size and intensity and by the subject on both dark spots intensity and skin tone.

Spectrophotometer readings Dermatologist evaluation

**

*

0%

2%

4%

6%

Normal skin Dyschromicskin

% o

f cha

nge

vs b

asel

ine

Skin Lightening Efficacy on normal and dyschromic skin

Week 4

Week 8

Week 12

* p<0.05

Uniformization of skin toneTFC-1067 (0.2%) vs Hydroquinone (2%)

0%

30%

60%

HQ (2%) TFC- 1067 (0.2%)% o

f cha

nge

vs b

asel

ine

Week 4

Week 8

Week 12

*

*

*

0%

10%

20%

30%

Spot Sizereduction

Spotlightening

% o

f cha

nge

vs b

asel

ine

Efficacy on dark spots

Week 4

Week 8

Week 12

* p<0.05

Subject evaluation

*

**

0%

10%

20%

30%

Spotlightening

Skin toneclarity

% o

f cha

nge

vs b

asel

ine

Lightening efficacy

Week 4

Week 8

Week 12

* p<0.05

Before

After

Sirona Biochem Corp.c/o WeWork 595 Burrard St. Vancouver, B.C., Canada,V7X 1L4Tel : 1-604-641-4466info@sironabiochem.com

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TFChem Subsidiary of Sirona BiochemVoie de l’innovationPharmaParc II27100 Val de Reuil FranceTel : +33 (0)232 090 116 contact@tfchemistry.com