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Nilotinib in Preventing Paclitaxel-Induced Peripheral Neuropathy in Patients With Stage I-III Breast Cancer

A Phase Ib Study of the Safety and Pharmacology of Nilotinib to Prevent Paclitaxel-Induced Peripheral Neuropathy in Patients With Breast Cancer

Status
Completed
Phases
Phase 1
Study type
Interventional
Source
ClinicalTrials.gov
Registry ID
NCT04205903
Enrollment
11
Registered
2019-12-20
Start date
2020-12-11
Completion date
2024-12-18
Last updated
2025-06-29

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Anatomic Stage I Breast Cancer AJCC v8, Anatomic Stage IA Breast Cancer AJCC v8, Anatomic Stage IB Breast Cancer AJCC v8, Anatomic Stage II Breast Cancer AJCC v8, Anatomic Stage IIA Breast Cancer AJCC v8, Anatomic Stage IIB Breast Cancer AJCC v8, Anatomic Stage III Breast Cancer AJCC v8, Anatomic Stage IIIA Breast Cancer AJCC v8, Anatomic Stage IIIB Breast Cancer AJCC v8, Anatomic Stage IIIC Breast Cancer AJCC v8, Prognostic Stage I Breast Cancer AJCC v8, Prognostic Stage IA Breast Cancer AJCC v8, Prognostic Stage IB Breast Cancer AJCC v8, Prognostic Stage II Breast Cancer AJCC v8, Prognostic Stage IIA Breast Cancer AJCC v8, Prognostic Stage IIB Breast Cancer AJCC v8, Prognostic Stage III Breast Cancer AJCC v8, Prognostic Stage IIIA Breast Cancer AJCC v8, Prognostic Stage IIIB Breast Cancer AJCC v8, Prognostic Stage IIIC Breast Cancer AJCC v8

Brief summary

This phase Ib trial studies the side effects and best dose of nilotinib in preventing paclitaxel-induced peripheral neuropathy in stage I-III breast cancer patients who are receiving paclitaxel therapy. Chemotherapy is the usual or standard treatment for breast cancer. It kills cancer cells and lowers the chance that the cancer will come back. Sometimes, this treatment can cause numbness and tingling, especially in the hands and feet. This is called chemotherapy-induced peripheral neuropathy. This study aims to test the safety and effectiveness, both good and bad, of taking nilotinib in preventing chemotherapy-induced peripheral neuropathy.

Detailed description

PRIMARY OBJECTIVES: I. To determine the recommended phase 2 dose (RP2D) of nilotinib hydrochloride monohydrate (nilotinib) in combination with paclitaxel. II. To determine the toxicity profile (based on Common Terminology Criteria for Adverse Events \[CTCAE\] version \[v.\] 5.0) of nilotinib in combination with paclitaxel. SECONDARY OBJECTIVES: I. To determine the effect of paclitaxel on pharmacokinetics (PK) of nilotinib in the study population. II. To determine the effect of nilotinib on PK of paclitaxel in the study population. OUTLINE: This is a phase Ib, dose-escalation study of nilotinib hydrochloride monohydrate. PHASE Ib: Paclitaxel will be given weekly on days 1, 8, 15, of every 21 days, at a starting dose of 80mg/m2. Nilotinib will be given orally on cycle 1 Days 7, 14 once a day 24 hours prior to the paclitaxel infusion and again 30 minutes prior to the paclitaxel infusion on days 8, 15. During the cycle 1, PK will be obtained at baseline, during, and up to 24 hours after paclitaxel or nilotinib administration on the days 1, 7, 8. Patients will continue paclitaxel without nilotinib after cycle 1 as part of standard of care at the discretion of the treating investigator

Interventions

DRUGNilotinib

Given PO

Given PO on cycle 1 Days 7, 14, 15 once a day 24 hours prior to the paclitaxel infusion and again 30 minutes prior to the paclitaxel infusion on days 8, 15.

DRUGPaclitaxel

Given IV weekly on days 1, 8, 15, of every 21 days, at a starting dose of 80mg/m2

OTHERQuestionnaire Administration

Ancillary studies

Sponsors

National Cancer Institute (NCI)
CollaboratorNIH
Ohio State University Comprehensive Cancer Center
Lead SponsorOTHER

Study design

Allocation
RANDOMIZED
Intervention model
PARALLEL
Primary purpose
TREATMENT
Masking
DOUBLE (Subject, Investigator)

Eligibility

Sex/Gender
ALL
Age
18 Years to No maximum
Healthy volunteers
No

Inclusion criteria

* Men or Women with a known diagnosis of breast cancer stages I-III. * Be eligible for weekly or dose dense single agent paclitaxel therapy based on physician assessment. * Have an Eastern Cooperative Oncology Group (ECOG) performance status =\< 2 * Patients with ECOG scores of 3 or greater typically do not receive chemotherapeutic intervention. * Leukocytes \>= 2,000/uL. * Absolute neutrophil count \>= 1,500/uL. * Platelets \>= 100,000/uL. * Total bilirubin =\< upper limit of normal (ULN). * Aspartate aminotransferase (AST) (serum glutamic oxaloacetic transaminase \[SGOT\])/alanine aminotransferase (ALT) (serum glutamate pyruvate transaminase \[SGPT\]) =\< 2.5 x institutional upper limit of normal. * Creatinine within normal institutional limits OR \>= 50 mL/min for patients with creatinine levels above institutional normal. * Corrected QT interval (QTc) \< 450 milliseconds. * If a female subject is with child bearing potential, she must have a negative pregnancy test at screening. * Female subjects of child-bearing potential and men must agree to use adequate contraception prior to study entry, for the duration of study participation and for 3 months after completion of study treatment administration. Adequate contraception includes methods such as oral contraceptives, double barrier method (condom plus spermicide or diaphragm), or abstaining from sexual intercourse. * Be willing and able to understand and sign the written informed consent document. * Demonstrate adequate electrolyte values as defined below. Hypokalemia and/or hypomagnesemia must be corrected prior to initiating nilotinib: * Calcium 8.6-10.5mg/dL * Magnesium 1.6-2.6mg/dL

Exclusion criteria

* Known distant metastatic disease. * Is HER2+ and is receiving paclitaxel in conjunction with trastuzumab +/- pertuzumab. * Has experienced \> grade 1 neuropathy during previous therapies for early stage breast cancer. * Has experienced prior treatment-related toxicities that have not recovered to grade 1 or less (except for alopecia). * Has a history of grade 3-4 immediate hypersensitivity reaction to paclitaxel. * Has a history of clinically significant allergic reactions attributed to compounds of similar chemical or biologic composition to nilotinib or paclitaxel. * Has uncontrolled intercurrent illness including, but not limited to, ongoing or active infection, symptomatic congestive heart failure, unstable angina pectoris, cardiac arrhythmia, or psychiatric illness/social situations that would limit compliance with study requirements. * Is currently pregnant or breast feeding as there is an unknown but potential risk for adverse events in nursing infants secondary to treatment of the mother with nilotinib and paclitaxel. * Has any other medical or psychiatric condition that in the opinion of the investigator would make the study therapy unsafe for the patient. * Has gastrointestinal (GI) disorders or impairment of GI function that is likely to significantly alter the absorption of nilotinib * Has a marked baseline abnormal heart rhythm such as prolongation of QT/QTc interval (e.g., repeated demonstration of a QTc of \> 450msec) * Has a history of additional risk factors for TdP (e.g., heart failure, hypokalemia, hypomagnesemia, family history of Long QT Syndrome) * Uses potent CYP3A4 inhibitors (grapefruit juice, cyclosporine, ketoconazole, ritonavir) and if treatment cannot be either safely discontinued or switched to a different medication prior to starting nilotinib. * Has a known diagnosis of human immunodeficiency virus (HIV) and is currently taking combination antiretroviral therapy known or suspected to affect paclitaxel pharmacokinetics (PK). * Is concurrently using potent OATP1B1 inhibitors, including antibiotics (rifampicin, rifamycin SV, systemic fusidic acid, clarithromycin, erythromycin, roxithromycin, telithromycin), antiretrovirals (indinavir, saquinavir, ritonavir), cyclosporine, and gemfibrozil.

Design outcomes

Primary

MeasureTime frameDescription
Number of Adverse Events (Phase Ib)Up to 6 weeksWill be classified and attributed using National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) version (v)5.0 and will be summarized within and across dose levels using descriptive statistics. The overall number and percentage of patients experiencing adverse events (AEs) and toxicities will be summarized and reported as across all event types, non-hematologic AEs, hematologic AEs, and for each type. Specific focus will be in summarizing any neuropathy-related AEs by dose level and how this corresponds to our measures of OATP1B1 inhibition. All patients who have received at least one dose of the therapeutic agents will be evaluable for toxicity and tolerability.
Recommended Phase II Dose (RP2D) of Nilotinib in Combination With Paclitaxel (Phase Ib)Up to 6 weeksThe RP2D will be derived from an adaptive Bayesian method for dose-finding based on trade-offs between the probabilities of treatment efficacy and toxicity. In this design, treatment efficacy is defined as significant inhibition of OATP1B1 activity by nilotinib, without causing changes in the pharmacokinetic profiles of paclitaxel. Efficacy in this setting will be OATP1B1 inhibition as defined by a \>= 5-fold increase in the area under the curve (AUC) of GCDCA-S from pre- to post-treatment and/or detectable CDCA-24G levels post-treatment.

Other

MeasureTime frameDescription
Evaluate Effects of Nilotinib and Paclitaxel (Phase Ib) on Patients Through Pharmacokinetics (PK) for Clinical Significant Interactions.: Pre-dose, prior to starting paclitaxel (day 1, day 8), prior to starting nilotinib (day 8 only), immediately prior to end of paclitaxel, after paclitaxel on days 1 and 8 and pre-dose, after nilotinib on day 7.Will explore PK endpoints Area under the plasma concentration versus time curve (AUC)

Countries

United States

Participant flow

Pre-assignment details

Eleven participants enrolled in the study. One participant withdrew prior to be randomized to a dose level,, leaving ten participants who were randomized to the three dose levels.

Participants by arm

ArmCount
Dose Level 1 (100mg Nilotinib)
Patients receive paclitaxel IV on days 1, 8, and 15. Patients also receive nilotinib hydrochloride monohydrate PO on days 7, 8, 14, and 15 of cycle 1 and days -1, 1, 7, 8, 14, and 15 of cycle 2. Treatment repeats every 21 days for up to 4 cycles in the absence of disease progression or unacceptable toxicity. Nilotinib: Given PO Nilotinib Hydrochloride Monohydrate: Given PO on cycle 1 Days 7, 14, 15 once a day 24 hours prior to the paclitaxel infusion and again 30 minutes prior to the paclitaxel infusion on days 8, 15. Paclitaxel: Given IV weekly on days 1, 8, 15, of every 21 days, at a starting dose of 80mg/m2 Questionnaire Administration: Ancillary studies
5
Dose Level 2 (200mg Nilotinib)
Patients receive paclitaxel IV on days 1, 8, and 15. Patients also receive nilotinib hydrochloride monohydrate PO on days 7, 8, 14, and 15 of cycle 1 and days -1, 1, 7, 8, 14, and 15 of cycle 2. Treatment repeats every 21 days for up to 4 cycles in the absence of disease progression or unacceptable toxicity. Nilotinib: Given PO Nilotinib Hydrochloride Monohydrate: Given PO on cycle 1 Days 7, 14, 15 once a day 24 hours prior to the paclitaxel infusion and again 30 minutes prior to the paclitaxel infusion on days 8, 15. Paclitaxel: Given IV weekly on days 1, 8, 15, of every 21 days, at a starting dose of 80mg/m2 Questionnaire Administration: Ancillary studies
3
Dose Level 3 (300mg Nilotinib)
Patients receive paclitaxel IV on days 1, 8, and 15. Patients also receive nilotinib hydrochloride monohydrate PO on days 7, 8, 14, and 15 of cycle 1 and days -1, 1, 7, 8, 14, and 15 of cycle 2. Treatment repeats every 21 days for up to 4 cycles in the absence of disease progression or unacceptable toxicity. Nilotinib: Given PO Nilotinib Hydrochloride Monohydrate: Given PO on cycle 1 Days 7, 14, 15 once a day 24 hours prior to the paclitaxel infusion and again 30 minutes prior to the paclitaxel infusion on days 8, 15. Paclitaxel: Given IV weekly on days 1, 8, 15, of every 21 days, at a starting dose of 80mg/m2 Questionnaire Administration: Ancillary studies
2
Total10

Baseline characteristics

CharacteristicDose Level 1 (100mg Nilotinib)Dose Level 2 (200mg Nilotinib)Dose Level 3 (300mg Nilotinib)Total
Age, Categorical
<=18 years
0 Participants0 Participants0 Participants0 Participants
Age, Categorical
>=65 years
0 Participants0 Participants0 Participants0 Participants
Age, Categorical
Between 18 and 65 years
5 Participants3 Participants2 Participants10 Participants
Ethnicity (NIH/OMB)
Hispanic or Latino
0 Participants0 Participants0 Participants0 Participants
Ethnicity (NIH/OMB)
Not Hispanic or Latino
4 Participants3 Participants2 Participants9 Participants
Ethnicity (NIH/OMB)
Unknown or Not Reported
1 Participants0 Participants0 Participants1 Participants
Race (NIH/OMB)
American Indian or Alaska Native
0 Participants0 Participants0 Participants0 Participants
Race (NIH/OMB)
Asian
0 Participants0 Participants0 Participants0 Participants
Race (NIH/OMB)
Black or African American
1 Participants1 Participants0 Participants2 Participants
Race (NIH/OMB)
More than one race
0 Participants0 Participants0 Participants0 Participants
Race (NIH/OMB)
Native Hawaiian or Other Pacific Islander
0 Participants0 Participants0 Participants0 Participants
Race (NIH/OMB)
Unknown or Not Reported
0 Participants0 Participants0 Participants0 Participants
Race (NIH/OMB)
White
4 Participants2 Participants2 Participants8 Participants
Region of Enrollment
United States
5 participants3 participants2 participants10 participants
Sex: Female, Male
Female
5 Participants3 Participants2 Participants10 Participants
Sex: Female, Male
Male
0 Participants0 Participants0 Participants0 Participants

Adverse events

Event typeEG000
affected / at risk
EG001
affected / at risk
EG002
affected / at risk
deaths
Total, all-cause mortality
0 / 50 / 30 / 2
other
Total, other adverse events
5 / 53 / 32 / 2
serious
Total, serious adverse events
0 / 52 / 30 / 2

Outcome results

Primary

Number of Adverse Events (Phase Ib)

Will be classified and attributed using National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) version (v)5.0 and will be summarized within and across dose levels using descriptive statistics. The overall number and percentage of patients experiencing adverse events (AEs) and toxicities will be summarized and reported as across all event types, non-hematologic AEs, hematologic AEs, and for each type. Specific focus will be in summarizing any neuropathy-related AEs by dose level and how this corresponds to our measures of OATP1B1 inhibition. All patients who have received at least one dose of the therapeutic agents will be evaluable for toxicity and tolerability.

Time frame: Up to 6 weeks

ArmMeasureGroupValue (NUMBER)
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Otitis externa1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Anemia10 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Cardiac disorders - Other, specify1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Ear and labyrinth disorders - Other, specify1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Blurred vision1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Eye pain1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Watering eyes1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Constipation1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Diarrhea4 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Gastroesophageal reflux disease2 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Gastrointestinal disorders - Other, specify1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Mucositis oral4 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Nausea3 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Edema limbs1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Fatigue4 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Localized edema3 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Pain1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Mucosal infection2 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Injury, poisoning and procedural complications - Other, specify1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Alkaline phosphatase increased1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Lymphocyte count decreased2 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Neutrophil count decreased5 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)White blood cell decreased4 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Anorexia4 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Hyperglycemia3 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Hyperphosphatemia1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Arthralgia1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Bone pain1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Musculoskeletal and connective tissue disorder - Other, specify1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Myalgia3 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Dysgeusia2 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Headache4 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Nervous system disorders - Other, specify1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Paresthesia1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Peripheral sensory neuropathy5 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Anxiety1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Depression3 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Insomnia1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Allergic rhinitis4 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Dyspnea2 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Alopecia1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Bullous dermatitis1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Nail changes1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Pain of skin1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Palmar-plantar erythrodysesthesia syndrome2 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Rash maculo-papular1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Skin and subcutaneous tissue disorders - Other, specify5 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Flushing1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Hot flashes1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Hypertension1 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Dry mouth0 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Alanine aminotransferase increased0 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Aspartate aminotransferase increased Aspartate aminotransferase increased0 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Weight loss0 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Hypokalemia0 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Dizziness0 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Neuralgia0 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Peripheral motor neuropathy0 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Dry skin0 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Dysuria0 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Pruritus0 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Skin hyperpigmentation0 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Tinnitus0 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Abdominal pain0 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Vomiting0 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Breast infection0 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Platelet count decreased0 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Back pain0 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Joint range of motion decreased0 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Muscle cramp0 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Scoliosis0 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Extrapyramidal disorder0 Number of Events
Dose Level 1 (100mg Nilotinib)Number of Adverse Events (Phase Ib)Sleep apnea0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Aspartate aminotransferase increased Aspartate aminotransferase increased1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Neuralgia1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Hyperglycemia3 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Hyperphosphatemia0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Back pain0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Arthralgia1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Peripheral motor neuropathy1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Bone pain1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Musculoskeletal and connective tissue disorder - Other, specify0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Myalgia0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Dry skin1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Dysgeusia0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Headache1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Extrapyramidal disorder0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Nervous system disorders - Other, specify0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Dysuria1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Paresthesia1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Peripheral sensory neuropathy1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Joint range of motion decreased0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Anxiety1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Pruritus1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Depression1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Insomnia1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Allergic rhinitis0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Skin hyperpigmentation1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Dyspnea1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Alopecia0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Bullous dermatitis0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Tinnitus0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Nail changes0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Pain of skin0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Muscle cramp0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Palmar-plantar erythrodysesthesia syndrome1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Abdominal pain0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Rash maculo-papular0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Skin and subcutaneous tissue disorders - Other, specify0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Flushing0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Vomiting0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Hot flashes0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Scoliosis0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Anemia2 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Cardiac disorders - Other, specify0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Hypertension1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Ear and labyrinth disorders - Other, specify0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Blurred vision0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Eye pain0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Dry mouth1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Watering eyes0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Constipation1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Breast infection0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Diarrhea0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Alanine aminotransferase increased1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Gastroesophageal reflux disease1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Gastrointestinal disorders - Other, specify0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Mucositis oral1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Anorexia0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Nausea2 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Edema limbs0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Fatigue2 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Weight loss1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Localized edema0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Pain2 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Platelet count decreased0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Mucosal infection0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Otitis externa0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Hypokalemia1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Injury, poisoning and procedural complications - Other, specify0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Alkaline phosphatase increased0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Lymphocyte count decreased1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Dizziness1 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Neutrophil count decreased0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)White blood cell decreased0 Number of Events
Dose Level 2 (200mg Nilotinib)Number of Adverse Events (Phase Ib)Sleep apnea0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Nausea1 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Anorexia0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Paresthesia4 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Aspartate aminotransferase increased Aspartate aminotransferase increased0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Hyperglycemia2 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Neuralgia0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Hot flashes0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Hyperphosphatemia0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Lymphocyte count decreased3 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Anemia2 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Arthralgia0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Vomiting4 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Edema limbs0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Bone pain0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Peripheral motor neuropathy0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Cardiac disorders - Other, specify0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Musculoskeletal and connective tissue disorder - Other, specify0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Back pain1 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Scoliosis1 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Dizziness0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Ear and labyrinth disorders - Other, specify0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Dysgeusia0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Dry skin1 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Hypertension0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Headache1 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Fatigue3 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Blurred vision1 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Nervous system disorders - Other, specify0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Sleep apnea1 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Injury, poisoning and procedural complications - Other, specify0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Dysuria0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Eye pain0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Peripheral sensory neuropathy0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Hypokalemia0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Localized edema0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Anxiety1 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Watering eyes0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Dry mouth0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Depression1 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Pruritus0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Weight loss0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Insomnia0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Joint range of motion decreased1 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Constipation1 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Allergic rhinitis0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)White blood cell decreased2 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Pain4 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Dyspnea3 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Skin hyperpigmentation0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Diarrhea4 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Alopecia0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Extrapyramidal disorder1 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Alkaline phosphatase increased0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Bullous dermatitis0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Platelet count decreased2 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Gastroesophageal reflux disease1 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Nail changes0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Tinnitus1 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Alanine aminotransferase increased1 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Pain of skin0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Mucosal infection0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Gastrointestinal disorders - Other, specify0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Palmar-plantar erythrodysesthesia syndrome0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Breast infection2 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Myalgia0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Rash maculo-papular3 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Abdominal pain1 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Mucositis oral1 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Skin and subcutaneous tissue disorders - Other, specify0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Muscle cramp1 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Neutrophil count decreased0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Flushing0 Number of Events
Dose Level 3 (300mg Nilotinib)Number of Adverse Events (Phase Ib)Otitis externa0 Number of Events
Primary

Recommended Phase II Dose (RP2D) of Nilotinib in Combination With Paclitaxel (Phase Ib)

The RP2D will be derived from an adaptive Bayesian method for dose-finding based on trade-offs between the probabilities of treatment efficacy and toxicity. In this design, treatment efficacy is defined as significant inhibition of OATP1B1 activity by nilotinib, without causing changes in the pharmacokinetic profiles of paclitaxel. Efficacy in this setting will be OATP1B1 inhibition as defined by a \>= 5-fold increase in the area under the curve (AUC) of GCDCA-S from pre- to post-treatment and/or detectable CDCA-24G levels post-treatment.

Time frame: Up to 6 weeks

Population: The 6 participants who completed study treatment were evaluated for this outcome.

ArmMeasureValue (NUMBER)
Dose Level 1 (100mg Nilotinib)Recommended Phase II Dose (RP2D) of Nilotinib in Combination With Paclitaxel (Phase Ib)NA milligrams
Other Pre-specified

Evaluate Effects of Nilotinib and Paclitaxel (Phase Ib) on Patients Through Pharmacokinetics (PK) for Clinical Significant Interactions.

Will explore PK endpoints Area under the plasma concentration versus time curve (AUC)

Time frame: : Pre-dose, prior to starting paclitaxel (day 1, day 8), prior to starting nilotinib (day 8 only), immediately prior to end of paclitaxel, after paclitaxel on days 1 and 8 and pre-dose, after nilotinib on day 7.

Source: ClinicalTrials.gov · Data processed: Feb 18, 2026