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MOA: inhibitor of enzyme mTOR by binding to intracellular protein FKBP-12; results in G1 growth arrest
TA: renal cell carcinoma, mantle cell lymphoma (off label)
SE: hyperlipidemia and hyperglycemia
Temsirolimus
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MOA: inhibitor of enzyme mTOR by binding to intracellular protein FKBP-12; results in G1 growth arrest
TA: renal cell carcinoma; pancreatic neuroendocrine tumors; oral treatment of subependymal giant cell astrocytoma (SEGA) associated with tuberous sclerosis; postmenopausal, HER2- breast cancer in combo with exemestane
AE: none
Everolimus
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MOA: bind to alpha-beta tubulin heterodimer on microtubules to stabilize them and block metaphase leading to apoptosis
TA: breast cancer, endometiral cancer (unlabeled), can be combined with capecitabine
AE: sensory peripheral neuropathies
Ixabepilone
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MOA: inhibit microtubule by binding to tubulin and arresting mitosis in metaphase
TA: gel for anogenital and perianal warts (condyloma acuminata warts)
AE: significant neuropathies and death if applied to multiple and widespread lesions
podophyllotoxin
-
MOA: complexes with topoisomerase II to produce ds-dna breaks (G2 phase)
TA: refractory testicular tumor, SCLC
AE: none; inc risk of secondary malignancies within 5-8 yrs
Etoposide
-
MOA: complexes with topoisomerase II to produce ds-dna breaks (G2 phase)
TA: childhood acute lymphoblastic leukemia (ALL); adult ALL and NHL (off label)
AE: none
Teniposide
-
MOA:intercalates with DNA forming adducts that act as alkylating agents when light activated
TA: repigmentation of idiopathic vitiligo (leukoderma); psoriasis nonresponsive to other therapies; cutaneous t-cell lymphoma; cervical dysplasia
AE: severe burns and blistering if post UVA light exposure too soon after therapy
Methoxsalen
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MOA: activates protein kinase isoforms, inducing apoptosis
TA: short course topical therapy of actinic keratosis; precancerous skin lesions (topical)
AE: erythema, peeling, crusting, irritation
ingenol
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MOA: unknown, not cytolytic; induces maturation of acute promyelocytic leukemia cells in culture
TA: induction of remission in pts with acute promyelocytic leukemia (APL)
AE: effects associated with high doses of Vit A (headache, fever, dryness); rapid leukocytosis, CV/resp multiorgan failure (Retinoic acid-APL syndrome)
Tretinoin
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MOA: modulates innate and adaptive immune response by suppressing leukocyte recruitment and t cell activation
TA: cutaneous lesions in pts with AIDS-related Kaposi's sarcoma; cutaneous T-cell lymphoma
AE: erythema/rash, burning pain, pruritus
Alitretinoin
-
MOA: binds and activates retinoid x receptor subtypes activating receptors that function as transcription factors to regulate cel differentiation and proliferation
TA: cutaneous t-cell lymphoma
AE: hyperlipid, hyperchol, hypothyroid
Bexarotene
-
MOA: photochemical elevation to excited state by laser light leads to radical initial and ischemic necrosis within tumor secondary to vascular occlusion - thromboxane A2
TA: photodynamic therapy in esophageal cancer, endobroncial NSCLC, Barrett's esophagus
AE: Many (CV, CNS, GI, Resp)
Porfimer sodium
-
MOA: transition state inhibition of adenosine deminase, inhibiting ribonucleotide reductase; antimetabolite
TA: hairy cell leukemia
AE: neurologic (nervousness, insomnia, depression, hallucinations)
Pentostatin
-
MOA: inhibits growth of malignant cells that are asparagine-dependent
TA: pediatric acute lymphocytic leukemia
AE: decreased Vit K dependent clotting factors leading to hemorrhage; hypersensitivity
Asparaginase
-
MOA: induces differention of APL cells by degrading PML-RAR alpha protein; induces apoptosis; inhibits angiogenesis
TA: induction of remission and consolidation of acute promyelocytic leukemia
AE: prolong QT interval, APL differentiation syndrome (rash, dyspnea, fluid retention, pleural or pericardial effusions); leukocytosis
Arsenic trioxide
-
MOA: binds to tubulin at the rhizoxin binding site to inhibit microtubule assembly, induce microtubule disassembly, disrupt mitosis
TA: combined with trastuzumab as T-DM1 in treatment of Her2+ breast cancer
AE: none listed
Maytansine
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