Delving into the Latest Updates on FIT-039 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

CDK9

Mechanism

CDK9 inhibitors(Cyclin-dependent kinase 9 inhibitors)

Therapeutic Areas

Infectious DiseasesSkin and Musculoskeletal Diseases

Active Indication

Warts

Inactive Indication

Uterine Cervical Dysplasia

Originator Organization

KinoPharma, Inc.

Active Organization

KinoPharma, Inc.

Inactive Organization-

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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Structure

Molecular FormulaC17H18FN3S

InChIKeyVRKZHYSJZOUICG-UHFFFAOYSA-N

CAS Registry1113044-49-7

Author: Shibuya, Mami ; Tanaka, Shiro ; Egawa, Gyohei ; Kusuba, Nobuhiro ; Kabashima, Kenji ; Okamoto, Natsuko ; Nomura, Takashi ; Hagiwara, Masatoshi ; Okuno, Aika ; Tada, Harue ; Ishikawa, Makiko ; Nakagawa, Takayuki ; Nakajima, Saeko ; Sumi, Eriko ; Inoue, Nana ; Toichi, Eiko ; Uozumi, Ryuji ; Shimizuhira, Chihiro ; Mitsuishi, Tsuyoshi

TRIAL DESIGNHuman papillomavirus infection causes verruca vulgaris. CDK9 inhibitor FIT039 inhibits DNA virus proliferation in animal models. We conducted a multicenter, single-blind, placebo-controlled, randomized phase I/II clinical trial evaluating the safety and efficacy of FIT039 against verruca vulgaris.METHODSTarget lesions were treated with liquid nitrogen once, and a FIT039 patch or placebo patch was applied for 14 days. The primary endpoint was lesion disappearance. The secondary endpoints were safety and changes in dimension, cross-sectional area, and the number of petechial lesions.RESULTSA total of 24 participants were randomly allocated to the FIT039 (n = 13, median age, 54 years) and placebo (n = 11, median age, 62 years) groups. Verruca vulgaris did not disappear. FIT039 decreased the dimension to 76% of the initial value on day 29, followed by an increase to 98% on day 57. Placebo showed a monotonic increase to 107% on day 57. Changes in the cross-sectional area and petechiae number were comparable between the groups.CONCLUSIONSNo drug-related adverse reactions occurred. FIT039 efficacy was not determined in this study.

01 Dec 2019·TrialsQ4 · MEDICINE

The efficacy of a cyclin dependent kinase 9 (CDK9) inhibitor, FIT039, on verruca vulgaris: study protocol for a randomized controlled trial

Q4 · MEDICINE

ArticleOA

Author: Nakagawa, Takayuki ; Nomura, Takashi ; Tada, Harue ; Toichi, Eiko ; Nakajima, Saeko ; Sumi, Eriko ; Kabashima, Kenji ; Egawa, Gyohei ; Uozumi, Ryuji ; Hagiwara, Masatoshi

BACKGROUNDHuman papilloma viruses (HPVs) infect squamous epithelial cells and form verrucous lesions, or warts. Besides the psychosocial problems caused by the disfiguring warts, a subset of HPVs can be the primary etiologic agent for malignancies such as cervical cancer. However, there is no curative antiviral therapy for HPV infection. We recently found that the viral RNA transcription of DNA viruses requires cyclin dependent kinase 9 (CDK9) in the host cells, and that FIT039, a specific inhibitor of CDK9, suppressed the proliferation of DNA viruses such as herpes simplex virus 1 (HSV-1), HSV-2, human adenovirus, human cytomegalovirus, hepatitis virus B, and HPVs. Here, we describe a protocol to evaluate the safety and antiviral effect of FIT039 on common warts in human skin.METHODS AND DESIGNA multi-institutional, single-blind, placebo-controlled randomized phase I/II clinical trial was designed to evaluate the safety and efficacy of FIT039 on common warts on the extremities. A total of 44 adults with a primary diagnosis of verruca vulgaris on the extremities without serious comorbidities will be randomized into either the intervention group with an FIT039-releasing transdermal patch or a control group for a duration of 14 days. Outcomes will be assessed at baseline and postintervention. Participants will be further assessed at 2 months follow-up. The primary endpoint for efficacy is the resolution of the warts. The safety endpoint is the incidence of adverse events and adverse drug reactions. The secondary endpoints are changes in the dimensions of the wart, the cross-sectional area of the wart, and the number of clots within the area of the wart.DISCUSSIONThis study is the first to assess the efficacy of FIT039 and will contribute to the development of antiviral agents that can cure refractory common warts in immunocompromised patients.TRIAL REGISTRATIONUMIN Clinical Trials, UMIN000029695 . Registered on 1 November 2017.

01 Jan 2019·Clinical Drug InvestigationQ4 · MEDICINE

Safety and Plasma Concentrations of a Cyclin-dependent Kinase 9 (CDK9) Inhibitor, FIT039, Administered by a Single Adhesive Skin Patch Applied on Normal Skin and Cutaneous Warts

Q4 · MEDICINE

Article

Author: Uozumi, Ryuji ; Sawada, Teruo ; Asada, Ryuta ; Hagiwara, Masatoshi ; Kabashima, Kenji ; Yonezawa, Atsushi ; Tada, Harue ; Amino, Yoko ; Nomura, Takashi ; Sumi, Eriko

BACKGROUNDCutaneous warts are caused by human papilloma virus (HPV) infection. FIT039, a specific inhibitor of CDK9, suppresses the proliferation of DNA viruses in vitro.PURPOSEWe evaluated the safety, plasma concentrations, and efficacy of FIT039 delivered by single application of an adhesive skin patch on normal back skin and cutaneous warts.PATIENTS AND METHODSIn this placebo-controlled, dose-escalation, open-label, two-cohort phase I/II clinical trial, after a single administration of a 1% FIT039 patch, 3% FIT039 patch, or placebo on back skin, patients with cutaneous warts were treated with cryotherapy followed by a 1% FIT039 patch for 24 h in the first cohort. In the second cohort, cutaneous warts were treated with cryotherapy followed by a 3% FIT039 patch for 24 h. Adverse events and adverse drug reactions, the concentrations of FIT039, and surface area of cutaneous warts were evaluated.RESULTSNeither irritant reactions nor symptoms related to FIT039 occurred when the FIT039 patches were applied to patients' backs or on warts in ten patients. The concentrations of FIT039 were under 0.1 ng/ml at every time point. The median wart surface area at 1 week after application of the 1% FIT039 patch was similar to baseline, while that of the 3% FIT039 patch was smaller than baseline.CONCLUSIONThe FIT039 patch showed no topical or systemic adverse reactions when applied on normal skin or cutaneous warts. The safety and good adherence of the FIT039 patch are encouraging and support further studies to evaluate the efficacy of FIT039 in patients with cutaneous warts.

100 Deals associated with FIT-039

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