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Icatibant

Phase 3

Angioedema | Small molecule | Immunology |Takeda Pharmaceutical Company Limited|Last Updated: Jun 11, 2021

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Trial Design

RandomizedDouble-BlindPLACEBO_CONTROLLED
Total Trials1
Total Enrollment84

FDA Designations

No designations recorded

Clinical trial landscape

Icatibant · 8 trials · 4 indications

Phase 3 7Phase 1 1
NCT03888755A Study of Icatibant for Acute Attacks of Hereditary Angioedema in Japanese ParticipantsHereditary Angioedema (HAE)
COMPLETED8 Analytics
NCT01919801Blinded Safety & Efficacy Placebo Controlled Study of Icatibant for Angiotensin Converting Enzyme Inhibitor Induced AngioedemaAngiotensin Converting Enzyme Inhibitor Induced Angioedema
COMPLETED118 Analytics
NCT01386658A Pharmacokinetic, Tolerability and Safety Study of Icatibant in Children and Adolescents With Hereditary AngioedemaHereditary Angioedema (HAE)
COMPLETED32 Analytics
NCT00997204EASSI - Evaluation of the Safety of Self-Administration With IcatibantHereditary Angioedema
COMPLETED151 Analytics
NCT00912093A Study of Icatibant in Patients With Acute Attacks of Hereditary Angioedema (FAST-3)Hereditary Angioedema
COMPLETED98 Analytics
NCT00500656Subcutaneous Treatment With Icatibant for Acute Attacks of Hereditary Angioedema (HAE)Hereditary Angioedema
COMPLETED85 Analytics
NCT00097695Subcutaneous Treatment With Icatibant for Acute Attacks of Hereditary AngioedemaAngioedema
COMPLETED84 Analytics
PHASE3COMPLETED
A Study of Icatibant for Acute Attacks of Hereditary Angioedema in Japanese Participants
Hereditary Angioedema (HAE)Unlock trial analytics
PHASE3COMPLETED
Blinded Safety & Efficacy Placebo Controlled Study of Icatibant for Angiotensin Converting Enzyme Inhibitor Induced Angioedema
Angiotensin Converting Enzyme Inhibitor Induced AngioedemaUnlock trial analytics
PHASE3COMPLETED
A Pharmacokinetic, Tolerability and Safety Study of Icatibant in Children and Adolescents With Hereditary Angioedema
Hereditary Angioedema (HAE)Unlock trial analytics
PHASE3COMPLETED
EASSI - Evaluation of the Safety of Self-Administration With Icatibant
Hereditary AngioedemaUnlock trial analytics
PHASE3COMPLETED
A Study of Icatibant in Patients With Acute Attacks of Hereditary Angioedema (FAST-3)
Hereditary AngioedemaUnlock trial analytics
PHASE3COMPLETED
Subcutaneous Treatment With Icatibant for Acute Attacks of Hereditary Angioedema (HAE)
Hereditary AngioedemaUnlock trial analytics
PHASE3COMPLETED
Subcutaneous Treatment With Icatibant for Acute Attacks of Hereditary Angioedema
AngioedemaUnlock trial analytics

Study Endpoints

Primary Endpoints

Time to Onset of Symptom Relief (TOSR)
Baseline up to 120 hours post-treatment

The TOSR was defined as a 50 percent (%) reduction from the pre-treatment score in the 3-symptom composite VAS score for non-laryngeal attacks and 5-symptom composite VAS score for laryngeal attacks. A VAS utilizes a scale consisting of a 100 millimeter (mm) horizontal line with extreme values at the beginning (0 mm = no symptom) and end (100 mm = worst possible symptom) of the line. The participant should draw a vertical line at the point along the scale that represents the current status of the measured symptom. Composite VAS scores were calculated as the average of VAS measurements for skin swelling, skin pain, and abdominal pain (3-symptom composite) for non-laryngeal attacks and for skin swelling, skin pain, abdominal pain, difficulty swallowing, and voice change (5-symptom composite) for laryngeal attacks.

Time to Meeting Discharge Criteria (TMDC)
Day 0 up to Day 5

TMDC was based on the investigator-assessed angioedema-associated upper airway symptom assessments. It was calculated from the time of study drug administration to the earliest time point at which the symptoms of difficulty breathing and difficulty swallowing were absent and the symptoms of voice change and tongue swelling were mild or absent and all subsequent assessments continued to satisfy these conditions. These symptoms were evaluated by the investigator using a 5-point grading scale (0=absent, 1=mild, 2=moderate, 3=severe, and 4=very severe). TMDC was analysed using Kaplan-Meier estimates.

Number of Participants With Treatment-emergent Adverse Events (TEAE) and Treatment-emergent Serious Adverse Events (TESAEs)
From start of study drug administration (Day 0) up to follow-up (Day 5)

An adverse event (AE) was any untoward medical occurrence in a participant who received study drug without regard to possibility of causal relationship. An serious adverse event (SAE) was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. TEAEs were defined as adverse events/serious adverse events that started or worsened after the study drug treatment.

Number of Participants With Treatment Emergent Injection Site Reaction
Day 0 to Day 5

Injection site reaction included erythema, swelling, cutaneous pain, burning sensation, itching and warm sensation

Number of Participants With Clinically Significant Changes in Laboratory Evaluation, Vital Signs, Electrocardiogram (ECG) and Physical Examination
Day 0 to Day 5

During laboratory evaluation, serum chemistry and hematology blood tests, and urinalysis were performed. Vital signs parameters included evaluation of pulse rate and systolic and diastolic blood pressure. Standard 12-lead ECGs were performed and ECG recordings were read locally at the study site by a cardiologist. Physical examination was performed with examination of major body systems per routine clinical practice.

Time to Peak Concentration (Tmax) of a Single Subcutaneous (SC) Dose of Icatibant
Pre-dose; 0.25, 0.5, 0.75, 1, 2, 4 and 6 hours post-dose on Day 1

Time to peak concentration (Tmax) of a single SC dose of icatibant was reported.

Maximum Plasma Concentration (Cmax) of a Single Subcutaneous (SC) Dose of Icatibant
Pre-dose; 0.25, 0.5, 0.75, 1, 2, 4 and 6 hours post-dose on Day 1

Maximum plasma concentration (Cmax) of a single SC dose of icatibant was reported.

Total Plasma Clearance (CL/F) of a Single Subcutaneous (SC) Dose of Icatibant
Pre-dose; 0.25, 0.5, 0.75, 1, 2, 4 and 6 hours post-dose on Day 1

Total plasma clearance (CL/F) of a single SC dose of icatibant was reported.

Area Under the Plasma Concentration-time Curve From Time Zero to 4 Hours Post-dose (AUC0-4) of a Single Subcutaneous (SC) Dose of Icatibant
Pre-dose; 0.25, 0.5, 0.75, 1, 2, and 4 hours post-dose on Day 1

Area under the plasma concentration-time curve from time zero to 4 hours post-dose (AUC0-4) of a single SC dose of icatibant was reported.

Area Under the Plasma Concentration-time Curve From Time Zero to 6 Hours Post-dose (AUC0-t) of a Single Subcutaneous (SC) Dose of Icatibant
Pre-dose; 0.25, 0.5, 0.75, 1, 2, 4 and 6 hours post-dose on Day 1

Area under the plasma concentration-time curve from time zero to 6 hours post-dose (AUC0-t) of a single SC dose of icatibant was reported.

Area Under the Plasma Concentration-time Curve From Time Zero to Infinity (AUC0-inf) of a Single Subcutaneous (SC) Dose of Icatibant
Pre-dose; 0.25, 0.5, 0.75, 1, 2, 4 and 6 hours post-dose on Day 1

Area under the plasma concentration-time curve from time zero to infinity (AUC0-inf) of a single SC dose of icatibant was reported.

Volume of Distribution (Vz/F) of a Single Subcutaneous (SC) Dose of Icatibant
Pre-dose; 0.25, 0.5, 0.75, 1, 2, 4 and 6 hours post-dose on Day 1

Volume of distribution (Vz/F) of a single SC dose of icatibant was reported.

Elimination Half-life (t1/2) of a Single Subcutaneous (SC) Dose of Icatibant
Pre-dose; 0.25, 0.5, 0.75, 1, 2, 4 and 6 hours post-dose on Day 1

Elimination half-life (t1/2) of a single SC dose of icatibant was reported.

Number of Participants With Clinically Significant Changes in Vital Signs
Pre-dose up to 97 days post-dose

Vital signs included pulse rate, blood pressure, respiration rate, and temperature. The number of participants who reported clinically significant changes in vital signs were reported.

Number of Participants With Clinically Significant Changes in Electrocardiograms (ECGs)
6 - 8 hours post-dose on Day 1

A standard 12-lead ECG was performed after 10 minutes at rest when the participant was seated or supine following treatment. The number of participants who reported clinically significant changes in ECGs were reported.

Number of Participants With Clinically Significant Changes in Clinical Laboratory Evaluations
Pre-dose up to 97 days post-dose

Clinical laboratory evaluations included clinical chemistry (including liver function tests), hematology, urinalysis. The number of participants who reported clinically significant changes in clinical laboratory evaluations were reported.

Number of Participants Who Reported Presence of Anti-icatibant Antibodies
Pre-dose up to 97 days post-dose

The number of participants who reported anti-icatibant antibodies were reported.

Number of Participants With Adverse Events (AEs)
From the start of study drug administration up to 97 days post-dose

An AE was any noxious, pathologic, or unintended change in anatomical, physiologic, or metabolic function as indicated by physical signs, symptoms, or laboratory changes occurring in a clinical study, whether or not considered investigational product related.

Number of Participants Who Reported Injection Site Reactions (ISR) for Icatibant Exposure Number 1
1 h post-dose on Day 1 up to 9 days post-dose

The number of participants with injection site reactions (erythema, swelling, burning sensation, itching/pruritus, warm sensation, cutaneous pain, or other) that occured after initial icatibant administration was reported.

Number of Participants Who Reported Injection Site Reactions (ISR) for Icatibant Exposure Number 2 and 3
1 h post-dose up to 9 days post-dose

The number of participants with injection site reactions (erythema, swelling, burning sensation, itching/pruritus, warm sensation, cutaneous pain, or other) that occurred after subsequent icatibant administration by study-site personnel (health care practitioner \[HCP\] administration) or by caregiver/self (caregiver administration) was reported. In the below table, E-2 refers to icatibant exposure 2 and E-3 refers to icatibant exposure 3.

Number of Participants With Clinically Significant Changes in Reproductive Hormones
Pre-dose up to 97 days post-dose

Reproductive hormone levels of follicle-stimulating hormone (FSH), luteinizing hormone (LH), estradiol, and progesterone in females, and FSH, LH, and testosterone in males were measured. The number of participants with clinically significant changes in reproductive hormones was reported.

Number of Participants With Adverse Events in Self-treatment of Acute HAE Attacks With s.c. Injections of Icatibant
7 days from the beginning of each phase

Clinical safety of self-treatment of acute HAE attacks with s.c. injections of icatibant was assessed by calculating the number of AEs occurred during the study. Only those adverse events occurring up to the earlier of 7 days from the start of the naive phase, study discontinuation and start of the self-administration phase are assessed. The Local Tolerability Assessment tool was used. Subjects and Investigators graded erythema/reddening, swelling, burning, pruritus/itching, warm sensation, and skin pain on a 0 to 3 severity scale.

Time to Onset of Symptom Relief for an Acute Attack, as Assessed by the Patient
Up to 120 hours post-dose

Time to onset of symptom relief was calculated from study drug administration to onset of symptom relief, where onset of symptom relief was defined as the earliest of 3 consecutive measurements in which there was a 50% reduction from pretreatment in composite VAS score. Composite VAS score comprised 3 symptoms, including skin swelling, skin pain, and abdominal pain, for cutaneous and abdominal attacks and 5 symptoms, including skin swelling, skin pain, abdominal pain, difficulty swallowing, and voice change, for laryngeal attacks. Subjects who did not achieve symptom relief within the observation period were censored at the last observation time.

Time to Onset of Symptom Relief.
2 days

The primary efficacy endpoint was Time to onset of symptom relief (TOSR) following treatment with either icatibant or tranexamic acid. The median time to onset of symptom relief for the icatibant group was compared to the the median time to onset of symptom relief for the tranexamic acid group. TOSR was defined as the time between time of injection to time of first documented onset of symptom relief for the three primary symptoms: cutaneous swelling, cutaneous skin, and abdominal pain. The primary symptom was based on the type of attack. For abdominal attacks, the single primary symptom was abdominal pain. For cutaneous attacks, the single primary symptom was either skin swelling or skin pain, whichever was most severe.

Peak Plasma Concentration (Cmax) of Icatibant and Metabolites
Over 48 hours post-dose

Cmax is a term that refers to the maximum (or peak) concentration that a drug achieves in the body after the drug has been administrated.

Time to Peak Plasma Concentration (Tmax) of Icatibant and Metabolites
Over 48 hours post-dose

Tmax is the time after administration of a drug when the maximum plasma concentration in the body is reached.

Drug Concentration Half-Life (T1/2) of Icatibant and Metabolites
Over 48 hours post-dose

The time it takes for the blood plasma concentration of a substance to halve.

Area Under the Plasma Concentration-time Curve (AUC) From Time Zero to Infinity (AUCinf) of Icatibant and Metabolites
Over 48 hours post-dose

AUCinf is the area under the plasma concentration versus time curve extrapolated from time 0 to infinity, calculated using the observed value of the last non-zero concentration. AUC can be used as a measure of drug exposure. It is derived from drug concentration and time so it gives a measure how much and how long a drug stays in a body.

Total Body Clearance (CL/F) of Icatibant
Over 48 hours post-dose

The rate at which a drug is removed from the body.

Area Under the Plasma Concentration-Time Curve From Time Zero to the Time of the Last Quantifiable Concentration (AUC0-t) of Icatibant and Metabolites
Over 48 hours post-dose

AUC0-t is the area under the plasma concentration versus time curve extrapolated from time 0 to to the last quantifiable concentration. AUC can be used as a measure of drug exposure. It is derived from drug concentration and time so it gives a measure how much and how long a drug stays in a body.

Secondary Endpoints

Time to Onset of Primary Symptom Relief (TOSR-P)
Baseline up to 120 hours post-treatment
Change From Baseline in the Composite Visual Analog Scale (VAS) Score
Baseline, 2, 4 and 8 hours post-treatment
Composite Symptom Score (SS) Assessed by Investigator
8 hours post dose
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Study Design & Arms

AllocationNA
MaskingNONE
ModelSINGLE_GROUP
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
IcatibantEXPERIMENTALParticipants with 1 acute non-laryngeal or laryngeal attack will receive a single icatibant 30 milligram (mg) subcutaneous (SC) injection in the abdominal area. A maximum of 3 SC injections (or 90 mg) of icatibant that are at least 6 hours apart can be given for treatment of an attack if, within 48 hours of the initial treatment, there is insufficient relief or worsening of symptoms.
PlaceboPLACEBO_COMPARATORPlacebo will be administered as a single subcutaneous injection
Icatibant- Naive Treatment PhaseEXPERIMENTALSingle subcutaneous injection of icatibant, 30 mg
icatibant- Self administration PhaseEXPERIMENTALSingle subcutaneous injection of icatibant, 30 mg
Randomized controlled -IcatibantEXPERIMENTALSubjects received S.C icatibant+ oral placebo Icatibant Form: solution for injection, 3 mL, 10 mg/mL Single dose: 30 mg (3 mL) Placebo Form: hard capsule Single dose: 2 capsules Frequency: 3 x 2 capsules for 2 days, taken orally, 6 to 8 hours apart
Randomized controlled-Tranexamic acidACTIVE_COMPARATORSubjects received oral Tranexamic acid+ S.C. placebo Tranexamic acid Form: over encapsulated film tablet Single dose: 1000 mg (2 capsules) Frequency: 3 x 2 capsules for 2 days, taken orally, 6 to 8 hours apart Placebo Form: solution for injection, matched to icatibant for injection Single dose: 3 mL Frequency: one subcutaneous injection in the abdominal region
Controlled Open-label / laryngeal attackEXPERIMENTALPatients with laryngeal symptoms at the baseline were not randomised but treated with icatibant open label during the controlled phase.
Untreated patients at the baselineEXPERIMENTALPatients who were screened and found eligible but did not experience an angioedema attack, or had an attack that was not severe enough to merit treatment while the controlled phase was ongoing were treated in the open label phase with icatibant
Icatibant- RandomizedEXPERIMENTALPatients who were randomized to icatibant in the controlled phase after they had an eligible first in-study attack.
Placebo-RandomizedPLACEBO_COMPARATORPatients who were randomized to placebo in the controlled phase after they had an eligible first in-study attack.
Icatibant (30 mg)EXPERIMENTAL30mg dose of icatibant is administered as a single subcutaneous injection in the abdominal area

Interventions

NameTypeDescription
IcatibantDRUGParticipants will receive icatibant 30 mg SC injection in the abdominal area.
PlaceboDRUG -
Tranexamic AcidDRUGover encapsulated film tablet an anti-fibrinolytic agent,is used in some European countries for the treatment of acute oedema episodes and the continuous prophylaxis of HAE.
Oral PlaceboDRUGhard capsule matched to tranexamic acid
S.C. PlaceboDRUGsolution for injection, matched to icatibant for injection
Icatibant (30 mg)DRUGOn Day 1, subjects will receive a single 30mg subcutaneous injection of icatibant in their abdominal area. Subjects will be discharged from the study on Day 3 after collection of study related assessments
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Eligibility Criteria

Age Range18 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites8

Inclusion Criteria: 1. The participant is in Japan and is Japanese; defined as born in Japan and having Japanese parents and Japanese maternal and paternal grandparents. 2. The participant is male or female and greater than or equal to (\>=) 18 years of age at the time of informed consent. 3. The p...

Countries:JapanUnited StatesCanadaIsraelUnited KingdomAustraliaAustriaColombiaGermanyHungaryItalySpainArgentinaDenmarkFranceSwitzerlandRomaniaRussiaSouth AfricaUkraine
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Frequently asked questions about Icatibant

What is Icatibant used for?

Icatibant is used for the treatment of acute attacks of hereditary angioedema (HAE), a rare genetic condition causing episodes of severe swelling. It is also being studied for angiotensin converting enzyme inhibitor induced angioedema and other forms of angioedema. The drug is administered subcutaneously.

Who makes Icatibant?

Icatibant is developed by Takeda Pharmaceutical Company Limited, which trades under the ticker TAK. Takeda is responsible for the clinical development and commercialization of the drug.

What phase is Icatibant in?

Icatibant is in Phase 3 clinical development for hereditary angioedema (HAE). It is an investigational drug and has not been approved by regulatory authorities. Multiple Phase 3 trials have been completed to evaluate its safety and efficacy.

What clinical trials is Icatibant in?

Icatibant has completed three clinical trials. Key studies include NCT00097695, a Phase 3 trial in 84 patients with acute attacks of hereditary angioedema in the United States, and NCT01386658, a Phase 3 pediatric study in 32 patients across multiple countries. A Phase 1 study in healthy Japanese volunteers (NCT02045264) and a Phase 3 Japanese study (NCT03888755) were also completed.

How does Icatibant work?

Icatibant is a small molecule that acts as a selective bradykinin B2 receptor antagonist. By blocking the bradykinin B2 receptor, it inhibits the effects of bradykinin, a peptide that increases vascular permeability and leads to swelling in hereditary angioedema. This mechanism helps reduce the severity of acute attacks.

Is Icatibant the same as Firazyr?

Icatibant is also known by the brand name Firazyr. Both names refer to the same drug substance, which is developed by Takeda. Firazyr is the commercial name used in marketing and prescribing information for icatibant.