PowerPoint Presentation


1Therapeutics Clinical Research, San Diego, CA; 2BioPharmX, Inc., Menlo Park, CA; 
3JDR Dermatology Research, LLC, Las Vegas, NV; 4The Acne Treatment and Research Center, Morristown, NJ

Poster presented at the 13th Winter Clinical Dermatology Conference; Maui, Hawaii; January 12th-17th, 2018.

Bhatia N1; Ahmadyar M1; Hansra H2; Del Rosso J3; Baldwin H4; Daniels AM2

Early Onset of Efficacy Using a 1% and 2% Topical Minocycline Gel 

for the Treatment of Rosacea: a Small Open Label Study

+ Subject-Rated Tolerance Score Scale

Results:  Rapid and Effective

In conclusion,

The rapid rate of improvement

has the potential to improve

treatment compliance and

improved patient satisfaction.

An important advantage of the topical

minocycline formulation – especially in

chronic conditions such as rosacea in

which long-term use is possible – may be

in reduction of risks associated with

systemic exposure to this antibiotic.

Introduction

This is the first report of successful treatment of rosacea with a novel topical 

minocycline gel.  The efficacy endpoints of reduction in number and severity of 

facial lesions were met and showed rapid onset. For both the 1% and 2% 

formulations, clinically meaningful improvements were reported after just four weeks 

of treatment. 

Additionally, the minocycline gel treatment had a good profile for safety and 

tolerability. The majority of subjects stated they would use the minocycline gel 

again.

The study’s small size and open-label single-center design must limit conclusions 

drawn but suggest that larger-scale testing is warranted.  Next-phase clinical trials 

are planned. 

Methods

This was a phase 2 open-label feasibility study of 1% and 2%

formulations of a novel topical minocycline gel for the treatment

of rosacea.

Rosacea is a common, chronic, and relapsing skin disorder that 

presents with a variety of clinical manifestations primarily on the 

central face1.  The papulopustular subtype forms acne-like 

inflammatory papules, pustules, and plaques.  Genetic, immune, 

inflammatory, vascular, and environmental mechanisms may 

contribute to its development2,3.  Because no cure has been 

identified, current treatments are generally used chronically or 

intermittently and aim to suppress its symptoms4.

Minocycline is effective as a first-line systemic therapy for

rosacea; it is thought that, like other tetracyclines, its anti-

inflammatory properties are responsible5. However, significant

side effects such as gastrointestinal distress and vertigo may

make long-term use of oral minocycline intolerable and chronic

use may contribute to resistance. Another form of delivery with

lower overall dosage and reduced systemic side effects is

needed.

The study medication is the first completely solubilized

minocycline gel for topical use. Its preliminary safety and efficacy

profiles have been demonstrated in extensive preclinical testing.

Additionally, it has completed phase 2a and 2b testing for the

treatment of acne vulgaris.

1. Webster GF. Rosacea. Med Clin North Am 2009; 93:1183.

2. Abram K, Silm H, Maaroos HI, Oona M. Risk factors associated with rosacea. J Eur Acad Dermatol Venereol 2010; 24:565.

3. Wilkin J, Dahl M, Detmar M, Drake L, Feinstein A, Odom R, Powell F. Standard classification of rosacea: Report of the National Rosacea

Society Expert Committee on the Classification and Staging of Rosacea. J Amer Acad Derm 2002; 46(4):584.

4. Maier LE. Management of rosacea. UpToDate January 2017.

5. Korting HC, Schollmann C. Tetracycline actions relevant to rosacea treatment. Skin Pharmacol Physiol 2009; 22:287.

At baseline, the 1% group had 24.0 (±13.8; SD) lesions.  At week 12, this reduced to 1.7 
(±2.9).  In the 2% group, the mean of 28.1 (±12.8) to 4.0 (±5.4).

Percentage of subjects with improvements or no change in investigator- and subject-rated cutaneous tolerance scores from Baseline to Week 12

Cutaneous Tolerability Ratings Are Favorable

» Open-label, single-site study 

» 20 adults with moderate-to-severe (Grade 3 or 4; IGA*) 

papulopustular rosacea

» 12 weeks of treatment evaluating 2 arms: 1% (n=10) 

and 2% (n=9 [10 enrolled, 1 withdrawn]) formulations of 

topical minocycline gel

» Treatment assignment was non-randomized

» 2-grade reduction in IGA to clear or almost clear (0 or 1) 

from baseline to 12 weeks

» Change in lesion count from baseline to 12 weeks

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» Cutaneous tolerability (4-point severity scales, 

investigator- and subject-reported)

» Hematology & chemistry lab tests

» Treatment emergent AEs * Investigator Global Assessment (IGA); 
based on scale of 0 (clear) to 4 (severe)S

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Sponsored and supported by BioPharmX Corporation (Menlo Park, CA).
The topical minocycline gel is limited by federal or US law to investigational use only.

Percentage of Subjects with Improvements or No Change in 

Investigator- and Subject-rated Cutaneous Tolerance Scores from Baseline to Week 12

1%Topical Minocycline 

Gel (n=10)

2% Topical Minocycline 

Gel (n=9)

Combined Treatment 

Groups (n=19)

Investigator-reported

Erythema 100.0% 100.0% 100.0%

Scaling/peeling 100.0% 100.0% 100.0%

Edema 100.0% 100.0% 100.0%

Subject-reported

Burning 80.0% 77.8% 78.9%

Stinging 60.0% 77.8% 68.4%

Tightness 60.0% 77.8% 68.4%

Itching 70.0% 88.9% 78.9%

Topical minocycline gelThe study medication:

Strong 

Efficacy

» Stabilizes & solubilizes minocycline
» Delivered directly to affected facial skin
» Targeted penetration

Strong 

Safety Profile

» Low dose: 1% and 2% minocycline
» Minimizes side effects
» Low systemic exposure

» Rapidly absorbing
» Non-staining
» Non-oily
» Non-fluorescing
» Very high patient satisfaction 

in clinical trials

Positive Patient 

Experience

Percentage of subjects with improvements or no change in investigator- and 
subject-rated cutaneous tolerance scores from Baseline to Week 12

Satisfaction: Both 1% and 2% 
Formulations Show Potential for High 

Patient Compliance

1

2

3

4

5 
(most favorable)

Do you like the study medication?
Scale of 1 - 5

63% of subjects liked the study medication
(with a score of 4 or 5)

79% of subjects would use again

Good Safety Profile

» Generally safe and well tolerated

» No serious drug-related adverse events

» 3 adverse events were reported, but 

none were related to the study drug or 

study assessments 

» Lower molar abscess (n=1; 1% 

arm)

» Upper respiratory infection (n=1; 

1% arm)

» Contusion on nose (n=1; 2% arm)

» No clinically significant laboratory test 

findings were noted

-100%

-80%

-60%

-40%

-20%

0%
Baseline Week 4 Week 8 Week 12

Series1

Series2

-100%

-80%

-60%

-40%

-20%

0%
Baseline Week 4 Week 8 Week 12

Series1

Series2

1%; n=10

2%; n=9

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1%; n=10

2%; n=9

Baseline Week 4 Week 8 Week 12

1% 24.0 4.3 3.2 1.7

2% 28.1 11.9 6.6 4.0

Percentage Change from Baseline

Mean Numbers of Lesions

Baseline Week 4 Week 8 Week 12

1% 3.3 1.7 1.3 0.5

2% 3.4 1.9 1.3 0.8

Mean IGA Scores

Percentage Change from Baseline

Reduction in Number of Lesions Reduction in Severity of Lesions