Targeted Therapies & Kinase Inhibitors

Trastuzumab Injection (440mg with WFI) is a recombinant humanized IgG1 monoclonal antibody on the WHO Model List of Essential Medicines that specifically targets the extracellular domain IV of the Human Epidermal Growth Factor Receptor 2 (HER2 / ErbB2) protein. It blocks ligand-independent HER2 homodimerization and downstream PI3K/Akt survival signaling, prevents shedding of the HER2 extracellular domain, and flags HER2-overexpressing tumor cells for Antibody-Dependent Cellular Cytotoxicity (ADCC) mediated by natural killer (NK) cells. Indicated for adjuvant and metastatic HER2-overexpressing (IHC 3+ or FISH-amplified) breast cancer and HER2-positive metastatic adenocarcinoma of the stomach or gastroesophageal junction.

Bortezomib Injection (2mg, 2.5mg, 3.5mg) is a dipeptidyl boronic acid reversible inhibitor of the 26S proteasome on the WHO Model List of Essential Medicines. It binds to the chymotrypsin-like catalytic site of the 20S core particle, preventing degradation of ubiquitinated proteins. This leads to toxic accumulation of intracellular polyubiquitinated proteins, stabilization of I-kappa-B-alpha, blockade of nuclear factor-kappa B (NF-kB) activation, and activation of the unfolded protein stress response, selectively killing multiple myeloma cells. Indicated for the treatment of adult patients with multiple myeloma and mantle cell lymphoma.

Imatinib Mesylate Tablets (400mg) is a revolutionary first-generation small-molecule protein tyrosine kinase inhibitor on the WHO Model List of Essential Medicines. It binds selectively to the ATP-binding pocket of the BCR-ABL chimeric tyrosine kinase (Philadelphia chromosome t(9;22)), locking it into an inactive conformation and terminating aberrant downstream proliferation signaling. Also potently inhibits receptor tyrosine kinases for platelet-derived growth factor (PDGFR) and stem cell factor (c-KIT / CD117). Indicated for newly diagnosed and chronic phase Philadelphia chromosome-positive Chronic Myeloid Leukemia (Ph+ CML), Ph+ Acute Lymphoblastic Leukemia (ALL), and c-KIT-positive Gastrointestinal Stromal Tumors (GIST).

Lenalidomide Capsules (5mg, 10mg, 25mg) is a potent second-generation 4-amino-glutamyl analogue immunomodulatory drug (IMiD) on the WHO Model List of Essential Medicines. It binds directly to cereblon (CRBN), the substrate recognition component of the cullin-RING E3 ubiquitin ligase complex CRL4-CRBN, inducing selective ubiquitination and proteasomal degradation of lymphoid transcription factors IKZF1 (Ikaros) and IKZF3 (Aiolos). This causes direct multiple myeloma cell apoptosis, downregulates IRF4 and MYC, stimulates IL-2 production to activate NK and T-cells, and inhibits pro-angiogenic factors (VEGF, bFGF). Indicated in combination with dexamethasone for multiple myeloma, myelodysplastic syndrome (MDS) associated with deletion 5q, and relapsed mantle cell lymphoma.

Erlotinib Tablets (150mg) is an oral first-generation epidermal growth factor receptor (EGFR / HER1) tyrosine kinase inhibitor on the WHO Model List of Essential Medicines. It reversibly competes with ATP for binding to the intracellular kinase domain of EGFR harboring activating mutations (exon 19 in-frame deletions or exon 21 L858R point mutations), blocking autophosphorylation and downstream pro-survival RAS/RAF/MAPK signaling. Indicated for first-line and maintenance therapy of metastatic non-small cell lung cancer (NSCLC) with sensitizing EGFR mutations, and in combination with gemcitabine for locally advanced, unresectable pancreatic cancer.

Gefitinib Tablets (250mg) is an oral selective first-generation EGFR tyrosine kinase inhibitor on the WHO Model List of Essential Medicines. It competitively inhibits ATP binding at the tyrosine kinase catalytic domain of mutated EGFR (exon 19 deletion or exon 21 L858R substitution), arresting cell cycle progression and stimulating apoptosis in EGFR-addicted tumor cells. Indicated for first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have sensitizing EGFR mutations.

Rituximab Injection (100mg/10ml, 500mg/50ml) is a genetically engineered chimeric murine/human IgG1-kappa monoclonal antibody on the WHO Model List of Essential Medicines targeting the transmembrane CD20 antigen expressed on pre-B and mature B lymphocytes. Binding of rituximab to CD20 triggers complement-dependent cytotoxicity (CDC), antibody-dependent cellular cytotoxicity (ADCC), and direct structural apoptosis, rapidly clearing normal and malignant B-cells from circulation. Indicated for Non-Hodgkin Lymphoma (Diffuse Large B-Cell Lymphoma, Follicular Lymphoma), Chronic Lymphocytic Leukemia (CLL), Rheumatoid Arthritis refractory to anti-TNF agents, Granulomatosis with Polyangiitis (Wegener's), and Pemphigus Vulgaris.

Rituximab Injection (100mg/10ml, 500mg/50ml) is a genetically engineered chimeric murine/human IgG1-kappa monoclonal antibody on the WHO Model List of Essential Medicines targeting the transmembrane CD20 antigen expressed on pre-B and mature B lymphocytes. Binding of rituximab to CD20 triggers complement-dependent cytotoxicity (CDC), antibody-dependent cellular cytotoxicity (ADCC), and direct structural apoptosis, rapidly clearing normal and malignant B-cells from circulation. Indicated for Non-Hodgkin Lymphoma (Diffuse Large B-Cell Lymphoma, Follicular Lymphoma), Chronic Lymphocytic Leukemia (CLL), Rheumatoid Arthritis refractory to anti-TNF agents, Granulomatosis with Polyangiitis (Wegener's), and Pemphigus Vulgaris.

Dasatinib Tablets (20mg, 50mg, 70mg) is a second-generation dual BCR-ABL and SRC family tyrosine kinase inhibitor on the WHO Model List of Essential Medicines. It binds to both the active and inactive conformations of the BCR-ABL kinase domain with >300-fold higher potency than imatinib, overcoming most imatinib-resistant BCR-ABL kinase domain mutations (except the gatekeeper T315I mutation). Indicated for newly diagnosed Ph+ CML in chronic phase, and accelerated/blast phase CML or Ph+ ALL with resistance or intolerance to prior therapy including imatinib.

Lapatinib Tablets (250mg) is an oral dual tyrosine kinase inhibitor of both EGFR (ErbB1) and HER2/neu (ErbB2) on the PMBI formulary. It reversibly binds to the intracellular ATP-binding domain of both receptors, inhibiting receptor phosphorylation and shutting down downstream MAPK and PI3K/Akt survival cascades in HER2-overexpressing tumor cells. Able to cross the blood-brain barrier. Indicated in combination with capecitabine for advanced or metastatic HER2-positive breast cancer progressing after prior trastuzumab, anthracyclines, and taxanes, and with letrozole for hormone receptor-positive/HER2-positive breast cancer.

Nintedanib Soft Gelatin Capsules (100mg, 150mg) is an oral triple angiokinase inhibitor that targets receptor tyrosine kinases for vascular endothelial growth factor (VEGFR-1/2/3), fibroblast growth factor (FGFR-1/2/3), and platelet-derived growth factor (PDGFR-alpha/beta). In pulmonary fibrosis, it inhibits proliferation, migration, and transformation of lung fibroblasts into myofibroblasts, slowing the rate of pulmonary function decline (FVC loss). Indicated for Idiopathic Pulmonary Fibrosis (IPF), chronic fibrosing interstitial lung diseases with a progressive phenotype, systemic sclerosis-associated ILD, and in combination with docetaxel for advanced NSCLC of adenocarcinoma histology.

Pomalidomide Capsules (2mg) is a third-generation, highly potent immunomodulatory agent (IMiD) on the WHO Model List framework. It binds to cereblon with >10-fold higher affinity than lenalidomide, recruiting and degrading IKZF1/IKZF3 even in lenalidomide-refractory multiple myeloma clones, triggering enhanced myeloma apoptosis and T-cell co-stimulation. Indicated in combination with low-dose dexamethasone for patients with relapsed and refractory multiple myeloma who have received at least two prior therapies, including lenalidomide and a proteasome inhibitor.

Bortezomib Injection (2mg, 2.5mg, 3.5mg) is a dipeptidyl boronic acid reversible inhibitor of the 26S proteasome on the WHO Model List of Essential Medicines. It binds to the chymotrypsin-like catalytic site of the 20S core particle, preventing degradation of ubiquitinated proteins. This leads to toxic accumulation of intracellular polyubiquitinated proteins, stabilization of I-kappa-B-alpha, blockade of nuclear factor-kappa B (NF-kB) activation, and activation of the unfolded protein stress response, selectively killing multiple myeloma cells. Indicated for the treatment of adult patients with multiple myeloma and mantle cell lymphoma.

Bortezomib Injection (2mg, 2.5mg, 3.5mg) is a dipeptidyl boronic acid reversible inhibitor of the 26S proteasome on the WHO Model List of Essential Medicines. It binds to the chymotrypsin-like catalytic site of the 20S core particle, preventing degradation of ubiquitinated proteins. This leads to toxic accumulation of intracellular polyubiquitinated proteins, stabilization of I-kappa-B-alpha, blockade of nuclear factor-kappa B (NF-kB) activation, and activation of the unfolded protein stress response, selectively killing multiple myeloma cells. Indicated for the treatment of adult patients with multiple myeloma and mantle cell lymphoma.

Crizotinib Capsules (250mg) is an oral small-molecule receptor tyrosine kinase inhibitor targeting Anaplastic Lymphoma Kinase (ALK), ROS1, and hepatocyte growth factor receptor (HGFR / c-MET) on the WHO Model List framework. It selectively inhibits ATP binding to the chimeric EML4-ALK fusion kinase or ROS1 fusion protein, halting aberrant downstream signaling. Indicated for locally advanced or metastatic non-small cell lung cancer (NSCLC) that is ALK-positive or ROS1-positive as detected by an approved test.

Dasatinib Tablets (20mg, 50mg, 70mg) is a second-generation dual BCR-ABL and SRC family tyrosine kinase inhibitor on the WHO Model List of Essential Medicines. It binds to both the active and inactive conformations of the BCR-ABL kinase domain with >300-fold higher potency than imatinib, overcoming most imatinib-resistant BCR-ABL kinase domain mutations (except the gatekeeper T315I mutation). Indicated for newly diagnosed Ph+ CML in chronic phase, and accelerated/blast phase CML or Ph+ ALL with resistance or intolerance to prior therapy including imatinib.

Dasatinib Tablets (20mg, 50mg, 70mg) is a second-generation dual BCR-ABL and SRC family tyrosine kinase inhibitor on the WHO Model List of Essential Medicines. It binds to both the active and inactive conformations of the BCR-ABL kinase domain with >300-fold higher potency than imatinib, overcoming most imatinib-resistant BCR-ABL kinase domain mutations (except the gatekeeper T315I mutation). Indicated for newly diagnosed Ph+ CML in chronic phase, and accelerated/blast phase CML or Ph+ ALL with resistance or intolerance to prior therapy including imatinib.

Dasatinib Tablets (20mg, 50mg, 70mg) is a second-generation dual BCR-ABL and SRC family tyrosine kinase inhibitor on the WHO Model List of Essential Medicines. It binds to both the active and inactive conformations of the BCR-ABL kinase domain with >300-fold higher potency than imatinib, overcoming most imatinib-resistant BCR-ABL kinase domain mutations (except the gatekeeper T315I mutation). Indicated for newly diagnosed Ph+ CML in chronic phase, and accelerated/blast phase CML or Ph+ ALL with resistance or intolerance to prior therapy including imatinib.

Lenalidomide Capsules (5mg, 10mg, 25mg) is a potent second-generation 4-amino-glutamyl analogue immunomodulatory drug (IMiD) on the WHO Model List of Essential Medicines. It binds directly to cereblon (CRBN), the substrate recognition component of the cullin-RING E3 ubiquitin ligase complex CRL4-CRBN, inducing selective ubiquitination and proteasomal degradation of lymphoid transcription factors IKZF1 (Ikaros) and IKZF3 (Aiolos). This causes direct multiple myeloma cell apoptosis, downregulates IRF4 and MYC, stimulates IL-2 production to activate NK and T-cells, and inhibits pro-angiogenic factors (VEGF, bFGF). Indicated in combination with dexamethasone for multiple myeloma, myelodysplastic syndrome (MDS) associated with deletion 5q, and relapsed mantle cell lymphoma.

Lenalidomide Capsules (5mg, 10mg, 25mg) is a potent second-generation 4-amino-glutamyl analogue immunomodulatory drug (IMiD) on the WHO Model List of Essential Medicines. It binds directly to cereblon (CRBN), the substrate recognition component of the cullin-RING E3 ubiquitin ligase complex CRL4-CRBN, inducing selective ubiquitination and proteasomal degradation of lymphoid transcription factors IKZF1 (Ikaros) and IKZF3 (Aiolos). This causes direct multiple myeloma cell apoptosis, downregulates IRF4 and MYC, stimulates IL-2 production to activate NK and T-cells, and inhibits pro-angiogenic factors (VEGF, bFGF). Indicated in combination with dexamethasone for multiple myeloma, myelodysplastic syndrome (MDS) associated with deletion 5q, and relapsed mantle cell lymphoma.

Nintedanib Soft Gelatin Capsules (100mg, 150mg) is an oral triple angiokinase inhibitor that targets receptor tyrosine kinases for vascular endothelial growth factor (VEGFR-1/2/3), fibroblast growth factor (FGFR-1/2/3), and platelet-derived growth factor (PDGFR-alpha/beta). In pulmonary fibrosis, it inhibits proliferation, migration, and transformation of lung fibroblasts into myofibroblasts, slowing the rate of pulmonary function decline (FVC loss). Indicated for Idiopathic Pulmonary Fibrosis (IPF), chronic fibrosing interstitial lung diseases with a progressive phenotype, systemic sclerosis-associated ILD, and in combination with docetaxel for advanced NSCLC of adenocarcinoma histology.

Pazopanib Tablets (200mg, 400mg) is an oral second-generation multi-tyrosine kinase inhibitor on the WHO Model List framework. It potently inhibits VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-alpha, PDGFR-beta, and c-KIT, starving tumors of blood supply. Indicated for advanced renal cell carcinoma (RCC) and advanced soft tissue sarcoma (STS) in patients who have received prior chemotherapy.

Pazopanib Tablets (200mg, 400mg) is an oral second-generation multi-tyrosine kinase inhibitor on the WHO Model List framework. It potently inhibits VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-alpha, PDGFR-beta, and c-KIT, starving tumors of blood supply. Indicated for advanced renal cell carcinoma (RCC) and advanced soft tissue sarcoma (STS) in patients who have received prior chemotherapy.

Sorafenib Tablets (200mg) is an oral multi-kinase inhibitor targeting both tumor cell proliferation and tumor angiogenesis on the WHO Model List of Essential Medicines. It potently inhibits intracellular serine/threonine kinases in the RAF/MEK/ERK pathway (CRAF, BRAF, mutant V600E BRAF) and cell-surface receptor tyrosine kinases including VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-beta, FLT3, and RET. Indicated for unresectable hepatocellular carcinoma (HCC), advanced renal cell carcinoma (RCC), and locally recurrent or metastatic progressive radioactive iodine-refractory differentiated thyroid carcinoma.

Sunitinib Capsules (12.5mg, 25mg) is an oral multi-targeted receptor tyrosine kinase inhibitor on the WHO Model List of Essential Medicines. It blocks signaling by VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-alpha, PDGFR-beta, c-KIT, FLT3, and RET, exerting powerful anti-angiogenic and direct antiproliferative effects. Indicated for advanced renal cell carcinoma (RCC), gastrointestinal stromal tumor (GIST) after disease progression on or intolerance to imatinib, and progressive neuroendocrine tumors of pancreatic origin (pNET).

Sunitinib Capsules (12.5mg, 25mg) is an oral multi-targeted receptor tyrosine kinase inhibitor on the WHO Model List of Essential Medicines. It blocks signaling by VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-alpha, PDGFR-beta, c-KIT, FLT3, and RET, exerting powerful anti-angiogenic and direct antiproliferative effects. Indicated for advanced renal cell carcinoma (RCC), gastrointestinal stromal tumor (GIST) after disease progression on or intolerance to imatinib, and progressive neuroendocrine tumors of pancreatic origin (pNET).

Thalidomide Capsules (50mg, 100mg, 200mg) is the prototypical immunomodulatory drug (IMiD) on the WHO Model List of Essential Medicines. It binds to cereblon (CRBN), promoting degradation of IKZF1 and IKZF3, and suppresses tumor necrosis factor-alpha (TNF-alpha) synthesis while inhibiting basic fibroblast growth factor (bFGF) and VEGF-induced angiogenesis. Indicated in combination with dexamethasone for newly diagnosed multiple myeloma and for acute treatment and maintenance of erythema nodosum leprosum (ENL / Hansen's disease).

Thalidomide Capsules (50mg, 100mg, 200mg) is the prototypical immunomodulatory drug (IMiD) on the WHO Model List of Essential Medicines. It binds to cereblon (CRBN), promoting degradation of IKZF1 and IKZF3, and suppresses tumor necrosis factor-alpha (TNF-alpha) synthesis while inhibiting basic fibroblast growth factor (bFGF) and VEGF-induced angiogenesis. Indicated in combination with dexamethasone for newly diagnosed multiple myeloma and for acute treatment and maintenance of erythema nodosum leprosum (ENL / Hansen's disease).

Thalidomide Capsules (50mg, 100mg, 200mg) is the prototypical immunomodulatory drug (IMiD) on the WHO Model List of Essential Medicines. It binds to cereblon (CRBN), promoting degradation of IKZF1 and IKZF3, and suppresses tumor necrosis factor-alpha (TNF-alpha) synthesis while inhibiting basic fibroblast growth factor (bFGF) and VEGF-induced angiogenesis. Indicated in combination with dexamethasone for newly diagnosed multiple myeloma and for acute treatment and maintenance of erythema nodosum leprosum (ENL / Hansen's disease).

Panitumumab Infusion (100mg, 400mg) is a recombinant, fully human IgG2 monoclonal antibody on the WHO Model List of Essential Medicines that binds specifically to the human Epidermal Growth Factor Receptor (EGFR / HER1). It competitively prevents binding of endogenous EGF and TGF-alpha, halting EGFR dimerization, receptor autophosphorylation, and downstream pro-proliferative intracellular cascades. Indicated for wild-type KRAS and NRAS (exon 2, 3, and 4) metastatic colorectal carcinoma (mCRC), as first-line therapy with FOLFOX, or as monotherapy following progression on oxaliplatin, irinotecan, and fluoropyrimidines.

Panitumumab Infusion (100mg, 400mg) is a recombinant, fully human IgG2 monoclonal antibody on the WHO Model List of Essential Medicines that binds specifically to the human Epidermal Growth Factor Receptor (EGFR / HER1). It competitively prevents binding of endogenous EGF and TGF-alpha, halting EGFR dimerization, receptor autophosphorylation, and downstream pro-proliferative intracellular cascades. Indicated for wild-type KRAS and NRAS (exon 2, 3, and 4) metastatic colorectal carcinoma (mCRC), as first-line therapy with FOLFOX, or as monotherapy following progression on oxaliplatin, irinotecan, and fluoropyrimidines.

Cabozantinib Tablets (20mg, 40mg, 60mg) is an oral multi-tyrosine kinase inhibitor targeting MET, VEGFR-1/2/3, RET, AXL, KIT, and TIE-2 on the PMBI formulary. Simultaneous inhibition of MET and AXL overcomes resistance pathways commonly triggered by VEGF-only blockade. Indicated for advanced renal cell carcinoma (RCC) following prior anti-angiogenic therapy, hepatocellular carcinoma (HCC) previously treated with sorafenib, and progressive medullary thyroid cancer.

Cabozantinib Tablets (20mg, 40mg, 60mg) is an oral multi-tyrosine kinase inhibitor targeting MET, VEGFR-1/2/3, RET, AXL, KIT, and TIE-2 on the PMBI formulary. Simultaneous inhibition of MET and AXL overcomes resistance pathways commonly triggered by VEGF-only blockade. Indicated for advanced renal cell carcinoma (RCC) following prior anti-angiogenic therapy, hepatocellular carcinoma (HCC) previously treated with sorafenib, and progressive medullary thyroid cancer.

Cabozantinib Tablets (20mg, 40mg, 60mg) is an oral multi-tyrosine kinase inhibitor targeting MET, VEGFR-1/2/3, RET, AXL, KIT, and TIE-2 on the PMBI formulary. Simultaneous inhibition of MET and AXL overcomes resistance pathways commonly triggered by VEGF-only blockade. Indicated for advanced renal cell carcinoma (RCC) following prior anti-angiogenic therapy, hepatocellular carcinoma (HCC) previously treated with sorafenib, and progressive medullary thyroid cancer.

Olaparib Tablets (100mg, 150mg) is a first-in-class oral poly(ADP-ribose) polymerase (PARP-1, PARP-2, PARP-3) inhibitor on the WHO Model List of Essential Medicines. It traps inactivated PARP enzymes at single-strand DNA breaks, transforming them into lethal double-strand breaks during replication. In homologous recombination deficiency (HRD) tumors (e.g., BRCA1 or BRCA2 germline or somatic mutations), cancer cells cannot repair double-strand breaks, triggering synthetic lethality and tumor apoptosis while sparing normal cells. Indicated for maintenance therapy in BRCA-mutated advanced ovarian cancer, HER2-negative metastatic breast cancer with germline BRCA mutation, metastatic pancreatic adenocarcinoma, and HRR gene-mutated metastatic castration-resistant prostate cancer.

Olaparib Tablets (100mg, 150mg) is a first-in-class oral poly(ADP-ribose) polymerase (PARP-1, PARP-2, PARP-3) inhibitor on the WHO Model List of Essential Medicines. It traps inactivated PARP enzymes at single-strand DNA breaks, transforming them into lethal double-strand breaks during replication. In homologous recombination deficiency (HRD) tumors (e.g., BRCA1 or BRCA2 germline or somatic mutations), cancer cells cannot repair double-strand breaks, triggering synthetic lethality and tumor apoptosis while sparing normal cells. Indicated for maintenance therapy in BRCA-mutated advanced ovarian cancer, HER2-negative metastatic breast cancer with germline BRCA mutation, metastatic pancreatic adenocarcinoma, and HRR gene-mutated metastatic castration-resistant prostate cancer.

Ibrutinib Capsules (140mg) is a first-in-class oral irreversible inhibitor of Bruton's Tyrosine Kinase (BTK) on the WHO Model List of Essential Medicines. It forms a covalent bond with cysteine 481 in the BTK active site, permanently disabling B-cell antigen receptor (BCR) signaling and halting malignant B-cell proliferation, survival, and homing to lymphatic niches. Indicated for Chronic Lymphocytic Leukemia (CLL) / Small Lymphocytic Lymphoma (SLL), Mantle Cell Lymphoma (MCL), Waldenstrom's Macroglobulinemia, and chronic Graft-versus-Host Disease (cGVHD).

Lenvatinib Capsules (4mg) is an oral receptor tyrosine kinase inhibitor that selectively inhibits VEGFR-1, VEGFR-2, and VEGFR-3, along with fibroblast growth factor receptors (FGFR-1, FGFR-2, FGFR-3, FGFR-4), PDGFR-alpha, KIT, and RET. Indicated for locally recurrent or metastatic, progressive radioactive iodine-refractory differentiated thyroid cancer, first-line treatment of unresectable hepatocellular carcinoma (HCC), and in combination with pembrolizumab for advanced endometrial carcinoma or advanced RCC.