PMID- 34713415
OWN - NLM
STAT- MEDLINE
DCOM- 20220216
LR  - 20220218
IS  - 1179-1888 (Electronic)
IS  - 1175-0561 (Print)
IS  - 1175-0561 (Linking)
VI  - 23
IP  - 1
DP  - 2022 Jan
TI  - Tapinarof Cream 1% for Extensive Plaque Psoriasis: A Maximal Use Trial on Safety, 
      Tolerability, and Pharmacokinetics.
PG  - 83-91
LID - 10.1007/s40257-021-00641-4 [doi]
AB  - BACKGROUND: Tapinarof is a novel topical therapeutic aryl hydrocarbon receptor 
      modulating agent in development for the treatment of psoriasis and atopic 
      dermatitis. OBJECTIVE: This multicenter, open-label trial assessed the safety, 
      tolerability, pharmacokinetics (PK), and efficacy of tapinarof cream 1% once 
      daily (QD) under maximal use conditions in extensive plaque psoriasis. METHODS: 
      Adults with a baseline Physician Global Assessment (PGA) score of >/= 3 and body 
      surface area (BSA) involvement >/= 20% received tapinarof cream 1% QD for 29 days. 
      Safety and tolerability assessments included adverse events (AEs) and local 
      tolerability scales. PK parameters were calculated using non-compartmental 
      analysis. Efficacy assessments included change in PGA, Psoriasis Area and 
      Severity Index score, and %BSA affected. RESULTS: Twenty-one patients were 
      enrolled. Common AEs were folliculitis, headache, back pain, and pruritus (none 
      led to discontinuation). Tapinarof plasma exposure was low, with the majority of 
      concentrations being below detectable limits. At day 29, 14 patients (73.7%) had 
      a >/= 1-grade improvement in PGA score and six patients (31.6%) had a >/= 2-grade 
      improvement; four patients (21.1%) achieved treatment success (PGA 0 or 1 and 
      >/= 2-grade improvement). CONCLUSION: Tapinarof cream 1% QD was well tolerated, 
      with limited systemic exposure and significant efficacy at 4 weeks in patients 
      with extensive plaque psoriasis. ClinicalTrials.gov Identifier NCT04042103.
CI  - (c) 2021. The Author(s).
FAU - Jett, John E
AU  - Jett JE
AUID- ORCID: 0000-0002-1940-457X
AD  - Dermavant Sciences, 3300 Paramount Parkway, STE 150, Morrisville, NC, 27560, USA.
FAU - McLaughlin, Michael
AU  - McLaughlin M
AUID- ORCID: 0000-0002-5628-1564
AD  - Dermavant Sciences, 3300 Paramount Parkway, STE 150, Morrisville, NC, 27560, USA.
FAU - Lee, Mark S
AU  - Lee MS
AUID- ORCID: 0000-0001-8281-0039
AD  - Progressive Clinical Research, San Antonio, TX, USA.
FAU - Parish, Lawrence Charles
AU  - Parish LC
AUID- ORCID: 0000-0002-4612-1508
AD  - Paddington Testing Company, Inc, Philadelphia, PA, USA.
FAU - DuBois, Janet
AU  - DuBois J
AUID- ORCID: 0000-0002-7487-7716
AD  - DermResearch, Inc, Austin, TX, USA.
FAU - Raoof, Tooraj Joseph
AU  - Raoof TJ
AUID- ORCID: 0000-0001-8634-4303
AD  - T. Joseph Raoof MD, Inc, Encino, CA, USA.
AD  - Encinitas Research Center, Encino, CA, USA.
FAU - Tabolt, Glenn
AU  - Tabolt G
AUID- ORCID: 0000-0002-9668-8270
AD  - Dermavant Sciences, 3300 Paramount Parkway, STE 150, Morrisville, NC, 27560, USA.
FAU - Wilson, Timothy
AU  - Wilson T
AUID- ORCID: 0000-0001-7085-7462
AD  - Dermavant Sciences, 3300 Paramount Parkway, STE 150, Morrisville, NC, 27560, USA.
FAU - Somerville, Matthew C
AU  - Somerville MC
AUID- ORCID: 0000-0001-5315-3164
AD  - Dermavant Sciences, 3300 Paramount Parkway, STE 150, Morrisville, NC, 27560, USA.
FAU - DellaMaestra, Wayne
AU  - DellaMaestra W
AUID- ORCID: 0000-0002-9559-9815
AD  - Dermavant Sciences, 3300 Paramount Parkway, STE 150, Morrisville, NC, 27560, USA.
FAU - Piscitelli, Stephen C
AU  - Piscitelli SC
AUID- ORCID: 0000-0002-4528-3273
AD  - Dermavant Sciences, 3300 Paramount Parkway, STE 150, Morrisville, NC, 27560, USA. 
      steve.piscitelli@dermavant.com.
LA  - eng
SI  - ClinicalTrials.gov/NCT04042103
PT  - Clinical Trial, Phase II
PT  - Journal Article
PT  - Multicenter Study
DEP - 20211028
PL  - New Zealand
TA  - Am J Clin Dermatol
JT  - American journal of clinical dermatology
JID - 100895290
RN  - 0 (Dermatologic Agents)
RN  - 0 (Resorcinols)
RN  - 0 (Stilbenes)
RN  - 84HW7D0V04 (tapinarof)
SB  - IM
MH  - Dermatologic Agents/pharmacokinetics/*therapeutic use
MH  - Humans
MH  - Psoriasis/*drug therapy
MH  - Resorcinols/pharmacokinetics/*therapeutic use
MH  - Severity of Illness Index
MH  - Skin Cream
MH  - Stilbenes/pharmacokinetics/*therapeutic use
PMC - PMC8776723
COIS- JEJ, WDM, MM, SCP, MCS, GT, and TW are employees of Dermavant Science, Inc. LCP 
      is an investigator for Dermavant Science, Inc. JDB is an investigator for 
      Allergan, Aclaris Therapeutics, Galderma USA, Brickell Biotech, Derma 
      Therapeutics, Endo International, LEO Pharmaceuticals, Cara Therapeutics, 
      Arcutis, Boston Pharmaceuticals, Atacama Therapeutics, Biofrontera, Bristol-Myers 
      Squibb, RAPT Therapeutics, NFlection Therapeutics, Incyte Corporation, and Bellus 
      Health. MSL is an investigator for Abbvie, Asana, Pfizer, Eli Lilly, AstraZeneca, 
      Leo, Arena, Dermira, Cara, Bellus, Foamix, Arcutis, Incyte, UCB, and Boehringer 
      Ingelheim. TJR has no conflicts of interest to disclose.
EDAT- 2021/10/30 06:00
MHDA- 2022/02/17 06:00
PMCR- 2021/10/28
CRDT- 2021/10/29 06:40
PHST- 2021/09/26 00:00 [accepted]
PHST- 2021/10/30 06:00 [pubmed]
PHST- 2022/02/17 06:00 [medline]
PHST- 2021/10/29 06:40 [entrez]
PHST- 2021/10/28 00:00 [pmc-release]
AID - 10.1007/s40257-021-00641-4 [pii]
AID - 641 [pii]
AID - 10.1007/s40257-021-00641-4 [doi]
PST - ppublish
SO  - Am J Clin Dermatol. 2022 Jan;23(1):83-91. doi: 10.1007/s40257-021-00641-4. Epub 
      2021 Oct 28.