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Tranexamic Acid
INCI Name

: Tranexamic acid

Synonyms

: m-tranexamic acid

Chemical Name

: trans-4-(aminomethyl)cyclohexanecarboxylic
acid

CAS No.

: 701-54-2

EINECS No.

: 214-818-2

Molecular
Formula

: C8H15NO2

Molecular
Weight

: 157.2

Chemical Class

: Amino acids

Main Functions

: Whitening agent; Skin roughness improving

agent

Structure:

COOH

CH2NH2

Typical Specification
Appearance
Solubility
pH
Related
substance
Impurity A
Impurity B
Any other
impurity
All other
Impurities
Bromic
MySkinRecipes

: A white crystalline powder

: Freely soluble in water and in glacial acetic acid, practically
insoluble in alcohol and in acetone
: 7.0-8.0

: 0.1%
: 0.2%
: 0.1%
: 0.2%
: Not more than 670ppm
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Assay

: 99.0-101.0%

Functions
1

Whitening and prevent pigmentation

Reduce or remove the pigmentation of skin
Prevent and/or treat pigmentations such as chloasmas, freckles, sunburn, dark skin
and melanoderma caused by a drug such as steroid

Minimize dark spot area due to sun exposure.

Anti-inflammation
Act on the chronic mild inflammatory condition at the sites of spots, to suppress
melanocyte activation

2 Inhibit or improve skin roughness

Restore damaged skin caused by UVA/UVB, pollution or other environmental factors.

Mechanism of whitening skin

Block melanin formation path induced by ultraviolet rays

Prevent melanin accumulation
Decreases melanocyte tyrosinase activity by preventing the binding of plasminogen to
the keratinocytes, which results in reduction of prostaglandins and arachidonic acid,
which are inflammatory mediators involved in melanogenesis.

Synergistic effects with other whitening ingredients

Tranexamic acid produces good synergistic effect when combined with ascorbic acid or its
derivatives such as magnesium ascorbyl phosphate, 3-O-ethyl ascorbic acid, disodium
adenosine triphophate, escinol (deacylated product of escin under hydrolysis by sodium
methylate), L-cysteine. Penetration enhancers helps the transdermic absorption of
tranexamic acid into spots.

Application
Tranexamic acid is suitable to all kinds of skin for removing pigmentation, whitening skin
and reducing spots, such as:
Pigmentation after sun exposure
Dark spots
Sensitive skin
Acne and inflammation
Postoperative care after laser, pulsed light treatment

Efficacy and Safety Comparison of Tranexamic Acid with

Other Whitening Ingredients

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Tranexamic acid is relatively stable to light, temperature, pH, and oxygen, and no special
protections are required to maintain its whitening effect, as compared with conventional
whitening ingredients. It is no irritant and no sensitive to skin and is safe for use in
whitening cosmetics.
Azelaic acid
Reduction of
melanin
Inhibit tyrosinase

L- ascorbic
acid

arbutin

Tranexaminc
acid

No irritation

Hypoallergenic

Anti-inflammatory

Use Level: 3% ( cosmetics - Thai FDA approved); 5.0% (quasi-drugs - Japan QD List)
[BACKGROUND]
1. Route of Melanin Formation
In melanocyte
: It is generally thought that biosynthesis of melanin occurs in a
cytoplasmic granule, melanosome, in the melanocyte via a complex
pathway in which tyrosine is oxidized by tyrosinase to cause
biosynthesis of dopa and dopaquinone, and the dopaquinone is
converted into indolequinone or the like due to auto-oxidation by
ultraviolet rays.
Outside of
: It has become clear that melanin, which so far has been considered
melanocyte
to be formed only in melanocytes, is also formed outside of
melanocytes.
It was found that the quick skin darkening under the sun is due to
the colorless pre-melanin DHICA (precursor of melanin) which has
accumulate in the epidermis is converted to melanin upon
exposure to ultraviolet A rays (long wave length).
When transparent DHICA solution was irradiated with UVA
equivalent to about 20 minutes of exposure to sunlight in the
summer, pre-melanin was converted to melanin in a short time.
Melanin and
: At the sites where spots develop, excessive melanin formation
inflammation
constantly takes place. It was found that inflammatory cells are
more abundant at the site of the spot than at the normal site (the
inflammation at the spot site is extremely slight and does not
manifest as redness, swelling or pain). It was also discovered that

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the number of activated melanocytes (melanin-producing cells) to
total melanocytes is higher at the spot site than at the normal site.
From these results, we may assume that melanocytes remain
activated because of "a chronic, mild inflammatory condition" and
excessive melanin formation thus persists at the site of the spot.
2. Pigmentations & melasma
Pigmentations such as chloasmas (or melasma), freckles, sunburn, dark skin and
melanoderma caused by a drug such as steroid are generated by excess deposition of
melanin pigment in the skin.
Melasma is an acquired symmetric hyperpigmentation characterized by irregular lightto gray-brown macules, especially on the face of women.
3. Accidental discovery of whitening effect by tranexamic acid
Tranexamic acid is an antifibrinolytic agent and is used to control excess bleeding. The
skin whitening effects of tranexamic acid was occasionally found when it was used as a
coagulant to treat aneurismal subarachnoid hemorrhage. And from then on, it was
used in physician's prescription to treat liver spots and pigmentation.
The most famous example is that tranexamic acid has been widely used in Shiseidos
whitening series products such as NAVISION IP Essence (TA), NAVISION TA Lotion,
NAVISION TA Essence and Melanoreduce EX
4. Clinical Uses of Tranexamic Acid
Bleeding and
: TA has been used clinically for over 30 years to treat abnormal
skin diseases
bleeding, as well as skin diseases such as eczema, hives,
drug-induced irritation, and toxicodermia, via internal
administration, and also orally to treat itching, swelling, and
erythema. It is a representative -amino aci-type anti-plasmin
agent that has a highly specific action on the fibrinolytic system,
blocking the conversion of plasminogen to plasmin by inhibiting
PA action through the formation of a reversible complex with
plasminogen. TA is also thought to form a reversible complex with
plasmin, inhibiting the reaction with fibrin.
Pigmentation
: Kondou et al. have published results from a clinical study
examining the effects of a tranexamic acid (TA) emulsion applied
topically to melasma and freckles. The study involved 33 subjects,
25 with melasma and 8 with freckles, who applied the TA emulsion
for five to eighteen weeks, after which their skin pigmentation was
visually assessed by a dermatologist.
Researchers found that the TA emulsion had improved the
pigmentation in 20 subjects with melasma (80%) and 6 subjects
(75%) with freckles. No side effect was recognized and thus the TA
emulsion was deemed safe. In regard to changes over the course of

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Melasma

the study, marked improvement was observed within eight weeks

for melasma but within 12 weeks for freckles; therefore,
improvement was considered to require at least two months of
topical application. The authors concluded the TA emulsion was an
effective cosmeceutical that provided a whitening effect on
melasma and freckles through inhibition of melanin synthesis. It
also prevented the appearance of new pigment spots and freckles.
: In an open pilot study, intradermal microinjection of tranexamic
acid was given to 100 women with melasma for 12 weeks. The
treatment was well tolerated, and 76.5% of the subjects reported
fair lightening of their melasma.