Details of the Drug Combinations

General Information of This Drug (ID: DM6QOVN)

• Drug Name: HKI-272 (DM6QOVN)
• Synonyms: Neratinib (ERBB2 inhibitor)

Indication

Breast cancer; ICD 11: 2C60-2C65; Status: Phase 3 [1]

• Therapeutic Class: Anticancer Agents
• Drug Type: Small molecular drug

List of Combinatorial Drugs (CBD) Containing This Drug

1 Investigative Drug Combination(s) Consisting of This drug

Normalized Drug Combination Synergy Score

Synergy scores were normalized using Min-Max Scaling to facilitate visual comparisons.

DrugCom Name	DrugCom ID	Component Drug	Indication	REF
HKI-272 + Ruxolitinib	DCPFKL6	Ruxolitinib	Hodgkin lymphoma (Cell Line: L-1236)	[2]

20 Clinical Trial Drug Combination(s) Consisting of This drug

DrugCom Name	DrugCom ID	Component Drug	Indication	REF
Fulvestrant + HKI-272	DC1FI0Q	Fulvestrant	Breast Neoplasms	[3]
HKI-272 + Vinorelbine	DC7E9KT	Vinorelbine	Breast Cancer	[4]
HKI-272 + Paclitaxel	DC8WXKO	Paclitaxel	Breast Cancer	[5]
HKI-272 + Temsirolimus	DCVRHD0	Temsirolimus	Breast Cancer	[6]
HKI-272 + Capecitabine	DCYKG3X	Capecitabine	Breast Cancer	[7]
HKI-272 + MK-4827	DC1A4BV	MK-4827	Advanced Solid Tumor	[8]
HKI-272 + Valproic Acid	DC35CCS	Valproic Acid	Solid Tumor, Adult	[9]
HKI-272 + Palbociclib	DCHG5OU	Palbociclib	Advanced Malignant Solid Neoplasm	[10]
HKI-272 + Capmatinib	DCTKV0R	Capmatinib	Metastatic Breast Cancer	[11]
HKI-272 + Everolimus	DCTX6VM	Everolimus	Advanced Malignant Solid Neoplasm	[10]
Ruxolitinib + HKI-272	DCYRPO5	Ruxolitinib	Metastatic Triple-Negative Breast Carcinoma	[12]
Trametinib + HKI-272	DCNKNAH	Trametinib	Advanced Malignant Solid Neoplasm	[10]
Fulvestrant + HKI-272	DC6U7W7	Fulvestrant	Stage IV (Metastatic) Breast Cancer	[13]
HKI-272 + Colestipol	DCASAWS	Colestipol	Early Stage HER2+ Breast Cancer	[14]
HKI-272 + Budesonide	DCM4LRJ	Budesonide	Early Stage HER2+ Breast Cancer	[14]
HKI-272 + Loperamide	DCS2X5I	Loperamide	HER2 Amplified Breast Cancer	[15]
HKI-272 + Colesevelam	DCUX4QR	Colesevelam	Early-stage Breast Cancer	[16]
HKI-272 + Temozolomide	DC9HUEN	Temozolomide	Glioblastoma	[17]
HKI-272 + Loperamide	DCCTNYH	Loperamide	Early Stage HER2+ Breast Cancer	[14]
HKI-272 + Temsirolimus	DCU2M04	Temsirolimus	HER2-mutant Non-Small Cell Lung Cancer	[18]

References

• [1] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021154)
• [2] Loss of function mutations in VARS encoding cytoplasmic valyl-tRNA synthetase cause microcephaly, seizures, and progressive cerebral atrophy.Hum Genet. 2018 Apr;137(4):293-303. doi: 10.1007/s00439-018-1882-3. Epub 2018 Apr 24.
• [3] ClinicalTrials.gov (NCT01670877) Neratinib +/- Fulvestrant in Metastatic HER2 Non-amplified But HER2 Mutant Breast Cancer
• [4] ClinicalTrials.gov (NCT00706030) Study Evaluating Neratinib (HKI-272) In Combination With Vinorelbine In Subjects With Solid Tumors And Metastatic Breast Cancer
• [5] ClinicalTrials.gov (NCT00915018) Study Evaluating Neratinib Plus Paclitaxel VS Trastuzumab Plus Paclitaxel In ErbB-2 Positive Advanced Breast Cancer
• [6] ClinicalTrials.gov (NCT01111825) Temsirolimus Plus Neratinib for Patients With Metastatic HER2-Amplified or Triple Negative Breast Cancer
• [7] ClinicalTrials.gov (NCT00741260) Study Evaluating The Combination Of Neratinib And Capecitabine In Solid Tumors And Breast Cancer
• [8] ClinicalTrials.gov (NCT04502602) Niraparib and Neratinib in Advanced Solid Tumors With Expansion Cohort in Advanced Ovarian Cancer
• [9] ClinicalTrials.gov (NCT03919292) Neratinib + Valproate in Advanced Solid Tumors, w/Expansion Cohort in Ras-Mutated Ca
• [10] ClinicalTrials.gov (NCT03065387) Neratinib and Everolimus, Palbociclib, or Trametinib in Treating Participants With Refractory and Advanced or Metastatic Solid Tumors With EGFR Mutation/Amplification, HER2 Mutation/Amplification, or HER3/4 Mutation or KRAS Mutation
• [11] ClinicalTrials.gov (NCT05243641) Neratinib and Capmatinib Combination (Phase Ib/II) in Metastatic Breast Cancer and Inflammatory Breast Cancer Patients With Abnormal HER-family and c-Met Pathway Activity as Measured by the CELsignia Signaling Analysis Test
• [12] ClinicalTrials.gov (NCT06008275) Neratinib in Combination With Ruxolitinib in Patients With mTNBC
• [13] ClinicalTrials.gov (NCT04901299) Fulvestrant + Neratinib In Breast Cancer
• [14] ClinicalTrials.gov (NCT02400476) An Open-Label Study to Characterize the Incidence and Severity of Diarrhea in Patients With Early-Stage HER2+ Breast Cancer Treated With Neratinib and Loperamide
• [15] ClinicalTrials.gov (NCT04366713) A Study to Characterize Colon Pathology in Patients With HER2 Amplified Breast Cancer Treated With Neratinib
• [16] ClinicalTrials.gov (NCT05252988) Three Antidiarrheal Strategies in HER2+/HR+ Early Breast Cancer Patients Treated With Extended Adjuvant Neratinib
• [17] ClinicalTrials.gov (NCT02977780) INdividualized Screening Trial of Innovative Glioblastoma Therapy (INSIGhT)
• [18] ClinicalTrials.gov (NCT01827267) Neratinib With and Without Temsirolimus for Patients With HER2 Activating Mutations in Non-Small Cell Lung Cancer