Causes of Drug Failure Summary

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What type of cell-mediated cytotoxicity can Fc receptor-bearing killer cells induce?

ADCC (correct)
Inflammation
Opsonization
Phagocytosis

What is the function of the fragment antigen-binding (Fab fragment) of an antibody?

Bind to antigens (correct)
Mediate biological activity
Activate the complement system
Interact with Fc receptors

Which region of an antibody interacts with cell surface receptors called Fc receptors?

Fc region (correct)
Fab fragment region
Heavy chain region
Light chain region

What is the Y-shaped structure of an antibody composed of?

One heavy chain and two light chains (D) Signup and view all the answers

What allows antibodies to carry out both antigen binding and biological activity mediation?

Fc region (A) Signup and view all the answers

In which year were César Milstein and Georges Köhler jointly awarded the Nobel Prize in physiology or medicine?

1984 (A) Signup and view all the answers

What is passive targeting in the context of site-specific delivery of protein drugs?

Utilizing the natural disposition pattern of the carrier for site-specific delivery (C) Signup and view all the answers

What is active targeting in the context of site-specific delivery of protein drugs?

Changing the natural disposition of the carrier with a homing device (B) Signup and view all the answers

What effect can monoclonal antibodies (MAbs) have on target cells?

Cause lysis of the target cell via the Fc receptor (B) Signup and view all the answers

What happens if a drug needs to reach a target site that is outside of the blood circulation?

It has to pass through the endothelial barrier (C) Signup and view all the answers

Under what conditions can endothelial permeability differ significantly?

In tumors and inflammation sites (B) Signup and view all the answers

What is the primary purpose of utilizing monoclonal antibodies as targeted therapeutic agents?

To affect the target cell function upon attachment (D) Signup and view all the answers

What is a common cause of a drug's failure to reach its target site?

The drug is rapidly eliminated through the kidneys or inactivated through metabolic action. (C) Signup and view all the answers

What is a potential side effect of a drug's largest fraction being distributed over non-target organs?

The drug exerts side effects at non-target organs. (D) Signup and view all the answers

What is a challenge associated with using therapeutic proteins as drugs?

Therapeutic proteins do not enter cells easily due to their high molecular weight and hydrophilic nature. (A) Signup and view all the answers

What is the purpose of a 'homing device' in site-specific delivery systems?

The homing device provides specificity and selects the assigned target site. (D) Signup and view all the answers

What is an example of a natural drug targeting device present in the human body?

Antibodies (A) Signup and view all the answers

What is the role of the antigen binding site in antibody-mediated drug targeting?

The antigen binding site serves as the homing device for specificity and target site selection. (A) Signup and view all the answers

What is a common issue with using murine antibodies for therapy?

They induce human anti-mouse antibodies (HAMA) (B) Signup and view all the answers

How can the problem of human anti-mouse antibodies (HAMA) be overcome?

By synthesizing smaller F(ab)2 or F(ab) fragments (A) Signup and view all the answers

What is the purpose of the Fc region in immunoglobulins?

To bear a highly conserved N-glycosylation site (D) Signup and view all the answers

What type of molecules are chimeric antibodies?

Partly human, partly murine (A) Signup and view all the answers

How can the development of humanized or human MAb minimize the induction of HAMA?

By minimizing the immunogenic potential of the Fc region (A) Signup and view all the answers

Which part of the antibody is responsible for inducing cytokine production?

The Fc region (D) Signup and view all the answers

What is the nature of the target site specificity of MAb raised against tumor structures?

Quantitative (D) Signup and view all the answers

What is the purpose of using cocktails of different MAb attached to the toxin?

To solve problems related to tumor cell heterogeneity (B) Signup and view all the answers

What is the mechanism of bystander effects?

The active part is released from the conjugate before being taken up by the target cell (D) Signup and view all the answers

What is the purpose of injecting free MAb prior to injection of the immunoconjugate?

To neutralize free circulating antigen (A) Signup and view all the answers

What is the size range of colloidal carrier systems proposed for protein targeting?

Diameters up to a few micrometers (D) Signup and view all the answers

What is the purpose of selecting other antigen/MAb combinations?

To avoid problems related to shedding or modulation (C) Signup and view all the answers