Related Experiment Video

Updated: Jan 21, 2026

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
13:22

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays

Published on: October 23, 2019

8.3K

First-in-Human, Healthy Volunteers Integrated Protocol of ETC-206, an Oral Mnk 1/2 Kinase Inhibitor Oncology Drug

Vincenzo Teneggi1, Veronica Novotny-Diermayr1, Lay Hoon Lee1

  • 1D3 (Drug Discovery and Development), A*STAR, Singapore, Singapore.

Clinical and Translational Science
|July 26, 2019
PubMed

Insights

Integrated clinical protocols and targeted oncology drug studies in healthy volunteers (HVs) increase early study complexity. This study details the results, benefits, and challenges of such a first-in-human (FIH) trial.

Area of Science:

  • Clinical Pharmacology
  • Drug Development
  • Oncology

Background:

  • Drug development faces challenges in efficiency and access to novel medicines.
  • Integrated clinical protocols and early studies of targeted oncology drugs in healthy volunteers (HVs) are increasingly complex.
  • The impact of these integrated approaches on scientific value and study implementation requires further investigation.

Purpose of the Study:

  • To describe the results, advantages, and limitations of an integrated clinical protocol for a first-in-human (FIH) study.
  • To evaluate the scientific value and implementation of a complex FIH study involving a targeted oncology drug in HVs.
  • To provide insights for designing and conducting similar demanding early clinical studies.

Main Methods:

  • Conducted a first-in-human (FIH) study in healthy volunteers (HVs).
  • Utilized an integrated clinical protocol for the administration of a targeted oncology drug (Mnk 1/2 small molecule inhibitor).
  • Analyzed study results, focusing on scientific value and operational implementation.

Main Results:

  • The integrated protocol facilitated the study of a targeted oncology drug in HVs.
  • Specific advantages and limitations of this approach were identified.
  • The study provided valuable data on the drug's profile and the protocol's feasibility.

Conclusions:

  • Integrated clinical protocols for targeted oncology drugs in HVs can be scientifically valuable and operationally feasible.
  • Careful design and consideration of potential challenges are crucial for demanding FIH studies.
  • This approach offers a framework for future complex early-phase drug development studies.

More Related Videos

Oral Biofilm Sampling for Microbiome Analysis in Healthy Children10:42

Oral Biofilm Sampling for Microbiome Analysis in Healthy Children

Published on: December 31, 2017

17.8K
Oral Combinational Antiretroviral Treatment in HIV-1 Infected Humanized Mice06:07

Oral Combinational Antiretroviral Treatment in HIV-1 Infected Humanized Mice

Published on: October 6, 2022

2.8K

Related Concept Videos

Oral Hypoglycemic Agents: α-Glucosidase Inhibitors01:19

Oral Hypoglycemic Agents: α-Glucosidase Inhibitors

α-glucosidase inhibitors, including acarbose (Precose), miglitol (Glyset), and voglibose (Voglib) (primarily available in Asia), are drugs that control blood sugar levels by delaying the digestion of starch and disaccharides. They achieve this by inhibiting α-glucosidase enzymes in the intestine, which slow the absorption of carbohydrates in the intestine, which in turn leads to a prolonged release of the glucoregulatory hormone GLP-1 from intestinal L-cells.
Acarbose and miglitol are...
535
Predicting Products: SN1 vs. SN202:27

Predicting Products: SN1 vs. SN2

Nucleophilic substitution reactions of alkyl halides can proceed via an SN1 or an SN2 mechanism. While in SN2 reactions, the nucleophile attacks the substrate simultaneously as the leaving group departs, in SN1 reactions, the substrate first dissociates to give the carbocation intermediate. Various factors such as the structure of the substrate, the strength of the nucleophile, and the nature of the solvent promote one mechanism over the other.
With increased substitution on the alkyl halide,...
15.9K
Protein Kinases and Phosphatases02:54

Protein Kinases and Phosphatases

Proteins undergo chemical modifications that trigger changes in the charge, structure, and conformation of the proteins. Phosphorylation, acetylation, glycosylation, nitrosylation, ubiquitination, lipidation, methylation, and proteolysis are various protein modifications that regulate protein activity. Such modifications are usually enzyme-driven.
Protein kinases
Many proteins in the cell are regulated by phosphorylation, the addition of a phosphate group. A family of enzymes called kinases...
15.0K
Non-Oral Extravascular Drug Absorption Routes01:15

Non-Oral Extravascular Drug Absorption Routes

Non-oral extravascular routes, which encompass sublingual, buccal, topical, intramuscular, and inhalation methods, primarily utilize passive diffusion to transport drugs into the systemic circulation. The absorption rates and effectiveness of these routes depend on the drug's physicochemical properties, as well as the patient's anatomical and pathophysiological state.
Lipophilic drugs that are stable at salivary pH (6) and exhibit minimal binding to the oral mucosa are absorbed more...
502
Antihypertensive Drugs: Direct Renin Inhibitors01:25

Antihypertensive Drugs: Direct Renin Inhibitors

The renin-angiotensin-aldosterone system (RAAS) is an intricate physiological pathway involving numerous enzymes and hormones, including renin, angiotensin-converting enzyme (ACE), angiotensin I and II, and aldosterone. Imbalances within this system increase the production of angiotensin II and aldosterone. Increased angiotensin II levels promote vasoconstriction and blood pressure elevation. Concurrently, higher aldosterone levels stimulate sodium and water reabsorption in the kidneys,...
1.3K
Antihypertensive Drugs: Angiotensin-Converting Enzyme Inhibitors01:30

Antihypertensive Drugs: Angiotensin-Converting Enzyme Inhibitors

Angiotensin-converting enzyme (ACE), a vital component of the renin-angiotensin-aldosterone system, is abundant in lung endothelial cells. ACE converts the inactive decapeptide, angiotensin I, into the active octapeptide, angiotensin II. This potent vasoconstrictor narrows blood vessels, increasing resistance to blood flow and elevating blood pressure. Angiotensin II also stimulates aldosterone production, encouraging kidney cells to reabsorb more sodium and water from urine, thereby increasing...
2.4K