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Drugs and Drug Candidates, Volume 3, Issue 2

2024 June - 8 articles

Cover Story: Currently available on-demand medications for hereditary angioedema attacks are administered intravenously or by injection and commonly associated with delayed or withheld treatment. We describe the discovery and development of a novel, orally administered treatment, sebetralstat, a potent and selective plasma kallikrein (PKa) inhibitor. Sebetralstat is rapidly absorbed, resulting in near-complete inhibition of circulating PKa in as little as 15 minutes. In the recently completed KONFIDENT Phase 3 trial (NCT05259917) sebetralstat was administered soon after the onset of attack (median, 41 minutes) and significantly reduced the time to beginning of symptom relief compared to placebo (median, 1.6 hrs versus 6.7 hrs; p < 0.001). A New Drug Application has been submitted to the US FDA. View this paper
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Articles (8)

  • Article
  • Open Access
5 Citations
3,687 Views
27 Pages

Effective therapies to treat skin hypopigmentation disorders caused by diminished melanin synthesis or export are limited due to potential side effects. In this work, we explored if cyclocurcumin (CYC), a curcuminoid found in minor amounts in turmeri...

  • Review
  • Open Access
18 Citations
9,331 Views
19 Pages

Two-Dimensional and Spheroid-Based Three-Dimensional Cell Culture Systems: Implications for Drug Discovery in Cancer

  • Anali del Milagro Bernabe Garnique,
  • Natália Sudan Parducci,
  • Lívia Bassani Lins de Miranda,
  • Bruna Oliveira de Almeida,
  • Leonardo Sanches and
  • João Agostinho Machado-Neto

The monolayer (two-dimensional or 2D) cell culture, while widely used, lacks fidelity in replicating vital cell interactions seen in vivo, leading to a shift toward three-dimensional (3D) models. Although monolayers offer simplicity and cost-effectiv...

  • Article
  • Open Access
2 Citations
2,406 Views
11 Pages

Essential Oil of Psidium glaziovianum Kiaersk Alleviates the Effects of Complete Freund’s Adjuvant (CFA)-Induced Arthritis by Regulating Inflammation and Oxidative Stress

  • Wêndeo Kennedy Costa,
  • João Victor de Oliveira Alves,
  • Beatriz Meyruze Barros Da Fonseca,
  • Valquíria Bruna Guimarães Silva,
  • Rafael Jardim Ferreira,
  • Thiago Henrique Napoleão,
  • Patrícia Maria Guedes Paiva,
  • Maria Tereza dos Santos Correia,
  • Alisson Macário de Oliveira and
  • Márcia Vanusa da Silva

Rheumatoid arthritis (RA) is a chronic and debilitating condition that affects a significant number of individuals worldwide. Unfortunately, the currently available therapeutic approaches often yield unsatisfactory results and may be accompanied by h...

  • Article
  • Open Access
2 Citations
2,922 Views
12 Pages

Preclinical Testing of Chronic ICA-1S Exposure: A Potent Protein Kinase C-ι Inhibitor as a Potential Carcinoma Therapeutic

  • Christopher A. Apostolatos,
  • Wishrawana S. Ratnayake,
  • Sloan Breedy,
  • Jacqueline Kai Chin Chuah,
  • James Alastair Miller,
  • Daniele Zink,
  • Marie Bourgeois and
  • Mildred Acevedo-Duncan

Protein kinase C-iota (PKC-ι) is an oncogene overexpressed in many cancer cells including prostate, breast, ovarian, melanoma, and glioma cells. Previous in vitro studies have shown that 5-amino-1-((1R,2S,3R,4R)-2-3-dihydroxy-4-(hydroxymethyl)cy...

  • Article
  • Open Access
2 Citations
2,947 Views
15 Pages

Toxicity and Teratogenic Potential of Piplartine from Piper tuberculatum Jacq. during Embryonic Development in Mice (Mus musculus)

  • Giulliano Rezende Silva,
  • Lívia Thaís Gontijo Miranda,
  • Shirley Aline da Costa Arteaga da Silva,
  • Laise Rodrigues de Andrade,
  • Natanael Carvalho de Souza,
  • Bruno Silva Sá,
  • Elivaldo Ribeiro de Santana,
  • Andreanne Gomes Vasconcelos,
  • Daniel Carneiro Moreira and
  • José Eduardo Baroneza
  • + 8 authors

Piplartine, also known as piperlongumine, is a natural and biologically active amide alkaloid found in various Piper species within the Piperaceae family. It possesses numerous beneficial properties that can be leveraged in the development of nanotec...

  • Article
  • Open Access
1 Citations
2,351 Views
11 Pages

Relaxant Activity of 4H-Pyran and 1,6-Dihydropyridine Derivatives on Isolated Rat Trachea

  • Samuel Estrada-Soto,
  • Soledad Alemán-Pantitlán,
  • Emmanuel Gaona-Tovar,
  • Fernando Hernández-Borja,
  • Yolanda Alcaraz,
  • Rafael Villalobos-Molina and
  • Miguel A. Vázquez

Derivatives of 4H-pyrans and 1,6-dihydropyridines have generated considerable attention due to their interesting biological and therapeutic values. Their pharmacological activities include vasorelaxant, anticarcinogenic, antimicrobial, and antioxidan...

  • Review
  • Open Access
4 Citations
8,597 Views
14 Pages

Sebetralstat: A Rapidly Acting Oral Plasma Kallikrein Inhibitor for the On-Demand Treatment of Hereditary Angioedema

  • Edward P. Feener,
  • Rebecca L. Davie,
  • Nivetha Murugesan,
  • Stephen J. Pethen,
  • Sally L. Hampton,
  • Michael D. Smith,
  • Paul K. Audhya and
  • Chris M. Yea

Sebetralstat is a novel, potent, and selective oral plasma kallikrein inhibitor drug candidate in clinical development for the on-demand treatment of hereditary angioedema (HAE). Upon binding, sebetralstat induces a conformational change in the activ...

  • Feature Paper
  • Review
  • Open Access
6 Citations
11,086 Views
17 Pages

Zilucoplan is a synthetic macrocyclic peptide approved by the Food and Drug Administration (FDA), in October 2023, for the treatment of generalized myasthenia gravis. It is considered as an orphan drug that causes the inhibition of terminal complemen...

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Drugs Drug Candidates - ISSN 2813-2998